Ligand source activities (1 row/activity)



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

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
11583188 139282 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 139282 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
44400674 125189 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 125189 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
17449900 139542 13 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139542 13 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
16094675 82157 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL216922 82157 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10359019 83325 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
CHEMBL219129 83325 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
10088259 101913 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 101913 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
44400585 68655 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68655 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
2 3261 23 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 3261 23 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 3261 23 None -2 7 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
11725531 54054 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 54054 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
6469918 79891 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79891 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
681 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
155559617 174884 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174884 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
44400585 68655 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68655 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
10378194 197765 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 197765 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
681 1465 72 None -7 15 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 1465 72 None -7 15 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 1465 72 None -7 15 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 1465 72 None -7 15 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 1465 72 None -7 15 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
10383724 83411 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219570 83411 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
16094681 83347 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 83347 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094684 136600 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
CHEMBL373964 136600 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
10065188 101604 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 101604 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
155568867 176154 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 176154 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
11221906 79911 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 79911 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
155536720 172187 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
11849262 80117 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213246 80117 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
2 3261 23 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3261 23 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3261 23 None -2 7 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
11849223 79847 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212189 79847 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
25142456 82406 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 82406 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44418745 83410 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219567 83410 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11325818 79788 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL211930 79788 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
10428669 83465 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
CHEMBL220015 83465 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
9835713 18486 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL127226 18486 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
10404144 205302 23 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 205302 23 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10361512 54439 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 54439 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
168285560 192918 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192918 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192918 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
5025739 169196 45 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 169196 45 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
44414898 138906 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL378302 138906 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10316440 141666 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL385417 141666 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094706 141909 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
CHEMBL386917 141909 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
10382581 101298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 101298 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
44400626 70402 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70402 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
11849638 80014 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212847 80014 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11772242 166287 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 166287 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
9861462 83334 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 83334 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
5025739 169196 45 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 169196 45 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
16094682 83479 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL220139 83479 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11280225 81096 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215569 81096 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
10430781 83278 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
CHEMBL218852 83278 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
11849734 80152 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213398 80152 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
10425450 201 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 201 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 201 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
44400519 133129 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 133129 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
681 1465 72 None -7 15 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1465 72 None -7 15 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1465 72 None -7 15 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1465 72 None -7 15 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1465 72 None -7 15 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
16094672 83269 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
CHEMBL218797 83269 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
11451703 139018 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 139018 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
10642239 186659 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 186659 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
119570 3159 96 None -11 11 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3159 96 None -11 11 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3159 96 None -11 11 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3159 96 None -11 11 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3159 96 None -11 11 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
16094666 81727 3 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10022369 83488 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL220192 83488 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
10665101 101525 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 101525 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
10404144 205302 23 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 205302 23 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
168268756 192764 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192764 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192764 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
16094678 83385 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
CHEMBL219417 83385 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
10045314 165983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL425288 165983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11175610 138125 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376639 138125 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6603820 95774 19 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 95774 19 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
3645619 3034 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 3034 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 3034 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
1353 1911 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
3559 1911 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
86 1911 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
CHEMBL54 1911 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
DB00502 1911 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
11849636 79846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL212188 79846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849225 80179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL213518 80179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094666 81727 3 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
CHEMBL216393 81727 3 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
16094705 83364 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
CHEMBL219340 83364 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
11325645 138677 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL377794 138677 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
44415054 81129 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL215670 81129 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
9997550 136599 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL373963 136599 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
10339711 83407 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
CHEMBL219564 83407 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
11849777 138632 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL377585 138632 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
2 3261 23 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3261 23 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3261 23 None -2 7 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
135407844 80084 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL213106 80084 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849639 80357 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL214343 80357 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11849816 78079 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 78079 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849822 80109 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL213208 80109 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
2 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
54562 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
CHEMBL240773 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
2 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
681 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1465 72 None -7 15 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
2 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
54562 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
CHEMBL240773 3261 23 None -2 7 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
11849637 79873 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212298 79873 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
9861462 83334 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 83334 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
681 1465 72 None -1 15 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 1465 72 None -1 15 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 1465 72 None -1 15 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 1465 72 None -1 15 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 1465 72 None -1 15 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
44400674 125189 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 125189 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
6469918 79891 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79891 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
2 3261 23 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
54562 3261 23 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
CHEMBL240773 3261 23 None -2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
10425450 201 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
11439072 168959 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL438961 168959 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
11849635 80379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
CHEMBL214440 80379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
681 1465 72 None -7 15 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1465 72 None -7 15 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1465 72 None -7 15 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1465 72 None -7 15 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1465 72 None -7 15 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
11849182 79869 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 79869 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
16094698 137868 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 137868 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
44417647 82161 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 82161 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 82161 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
11301354 141648 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385350 141648 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10617381 189686 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 189686 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44400553 70779 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70779 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849821 169300 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 169300 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44400553 70779 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70779 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
2 3261 23 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 3261 23 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 3261 23 None -2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
24878061 141411 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 141411 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
11849633 80578 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL214954 80578 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
9883554 165354 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 165354 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
11163137 141737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385826 141737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094671 83377 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219392 83377 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
10338536 82134 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL216721 82134 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
11269392 78010 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL209759 78010 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
11849634 141623 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL385230 141623 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849265 139540 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL379597 139540 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
11738945 79947 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212595 79947 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2653640 66219 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 66219 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
11849263 160937 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL411545 160937 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
681 1465 72 None -7 15 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 1465 72 None -7 15 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 1465 72 None -7 15 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 1465 72 None -7 15 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 1465 72 None -7 15 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
3303 2244 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 2244 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 2244 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
11849776 79772 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 79772 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
11739255 80018 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 80018 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10042205 136946 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
CHEMBL374326 136946 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
11256262 80001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 80001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
45361874 170021 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474734 79925 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL212490 79925 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
16094685 83631 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
CHEMBL220469 83631 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
11292299 79770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL211829 79770 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
6469693 79955 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79955 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
10593191 189108 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 189108 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
6466372 170062 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 170424 7 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094704 82156 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
CHEMBL216921 82156 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
11849224 80033 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212902 80033 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10616050 186646 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 186646 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
2 3261 23 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3261 23 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3261 23 None -2 7 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
10247720 13054 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 13054 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 13054 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10018402 82133 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
CHEMBL216719 82133 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
11324794 138259 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 138259 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094677 83336 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 83336 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11198974 80010 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212831 80010 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11849299 79395 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL211360 79395 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10405923 83403 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219551 83403 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849229 138174 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 138174 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11370781 79871 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 79871 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
11849820 77954 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209645 77954 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11849267 79872 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 79872 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
11849730 79949 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212607 79949 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
11849180 79808 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212028 79808 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
16094668 83326 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
CHEMBL219130 83326 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
10405922 83408 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219565 83408 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11849780 80183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL213558 80183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094683 137873 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
CHEMBL376196 137873 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
10042826 166139 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL426167 166139 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44415055 81141 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL215704 81141 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
155530763 171569 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171569 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44400519 133129 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 133129 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849684 80215 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213700 80215 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094674 141667 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
CHEMBL385418 141667 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
16094708 166073 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
CHEMBL425793 166073 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
11164276 79752 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 79752 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11199162 79859 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 79859 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10404935 83409 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
CHEMBL219566 83409 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
11849228 96416 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL261957 96416 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11151081 79795 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL211972 79795 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11849222 81219 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
CHEMBL215849 81219 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
228 445 28 None -1 20 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 445 28 None -1 20 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 445 28 None -1 20 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 445 28 None -1 20 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 445 28 None -1 20 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
11185987 80348 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 80348 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6469693 79955 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79955 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
11849179 81145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL215723 81145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
44418748 170459 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL444881 170459 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11450607 80172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL213486 80172 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
155552185 174061 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174061 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849819 80246 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL213828 80246 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11371795 79820 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212073 79820 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
10472323 83259 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL218761 83259 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
11849817 138930 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL378427 138930 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11771801 80029 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 80029 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10084583 104778 4 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104778 4 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
11849775 166196 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 166196 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849823 79605 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL211463 79605 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
11151919 80186 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213572 80186 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10385089 141730 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL385781 141730 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11849681 79801 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL211985 79801 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849181 80060 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 80060 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11211058 80334 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 80334 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11187957 139530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL379546 139530 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849778 81142 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 81142 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094709 83335 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL219181 83335 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
11473427 141507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL384529 141507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849184 80032 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212901 80032 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11849729 141902 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL386867 141902 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
11325334 80051 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 80051 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
2 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3261 23 None -2 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
3038495 708 37 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 708 37 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 708 37 None -91 7 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
11849688 79937 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212545 79937 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
2 3261 23 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
54562 3261 23 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
CHEMBL240773 3261 23 None -2 7 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
9975465 187651 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 187651 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
228 445 28 None 1 20 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 445 28 None 1 20 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 445 28 None 1 20 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 445 28 None 1 20 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 445 28 None 1 20 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
44301054 196148 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 196148 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
11983282 138943 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138943 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
10088811 83337 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL219186 83337 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
168285556 192917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
10064956 136386 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
CHEMBL373516 136386 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
10020098 83340 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219210 83340 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10335627 83387 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
CHEMBL219426 83387 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
11849298 79734 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL211623 79734 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
155513053 169698 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169698 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094697 137228 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
CHEMBL375120 137228 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
11200205 138911 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 138911 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094679 83277 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218851 83277 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11314352 79860 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212236 79860 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
109030515 175985 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175985 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094677 83336 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 83336 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849774 79870 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212290 79870 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849269 79552 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL211415 79552 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
71452737 79091 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113243 79091 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
44300865 201995 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 201995 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
16094681 83347 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 83347 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44418747 83378 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219394 83378 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
5311189 204841 11 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 204841 11 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
11336814 80101 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 80101 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
71456253 79092 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113244 79092 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
11739823 79771 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL211831 79771 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
11151920 80034 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 80034 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
109030343 170860 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170860 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11849735 138232 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377023 138232 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
10066168 161849 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
CHEMBL414706 161849 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
10428816 83348 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
CHEMBL219263 83348 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
11256583 168786 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL437493 168786 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
10024158 83341 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219211 83341 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
10404821 168680 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL436527 168680 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10383571 83258 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
CHEMBL218757 83258 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
11849687 80006 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212804 80006 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11724450 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44400626 70402 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70402 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
16094670 83455 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
CHEMBL219966 83455 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
11772112 168816 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 168816 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
11849779 79895 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL212393 79895 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
16094707 96726 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
CHEMBL264286 96726 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
16094667 81842 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
CHEMBL216450 81842 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
16094700 169723 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
CHEMBL443838 169723 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
3645619 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
975 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
CHEMBL45244 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
3645619 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
975 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
CHEMBL45244 3034 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
10737474 101353 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 101353 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
10473658 187193 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 187193 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
168285560 192918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
155515982 170010 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 170010 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849682 80319 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
CHEMBL214190 80319 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
11849736 138415 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 138415 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
11774041 80020 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL212872 80020 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
11394708 80082 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL213097 80082 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10359645 141536 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL384690 141536 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10385883 81571 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL216215 81571 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
10314506 168676 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
CHEMBL436491 168676 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
11772767 80002 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 80002 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
16094676 232 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 232 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 232 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
16094699 82145 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 82145 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
9859861 168080 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 168080 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10314824 35380 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 35380 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
11849818 77917 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209447 77917 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11983282 138943 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138943 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
16094665 83469 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL220083 83469 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10449865 83270 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218798 83270 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11416883 81130 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL215678 81130 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
16094676 232 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 232 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 232 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
15981509 141958 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 141958 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
11222637 79783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL211902 79783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
16094680 83375 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219389 83375 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
44393797 66360 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL185149 66360 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
11849266 81069 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 81069 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
11849781 80321 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL214197 80321 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
9995904 31219 4 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 31219 4 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
71458071 79500 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 79500 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
9926143 113526 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 113526 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
168285556 192917 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 192838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 192764 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192764 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192764 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 192764 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192764 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192764 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
45361874 170021 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
10021193 66363 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 66363 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
3303 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2244 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
109030343 170860 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170860 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 958 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 958 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 958 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 958 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 958 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
155513053 169698 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169698 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2244 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2244 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2244 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
16094666 81727 3 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
109030515 175985 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175985 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285556 192917 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
155536720 172187 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168277064 192838 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192838 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192838 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155536815 172207 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 172207 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
168268756 192764 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192764 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192764 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168285556 192917 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 192838 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192838 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192838 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155568411 176080 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 176080 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
155562395 175948 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175948 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
6466372 170062 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155563301 175250 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 175250 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
9907332 16396 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 16396 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
155530763 171569 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171569 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285560 192918 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192918 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192918 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
10425450 201 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
155511803 169605 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169605 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155516494 170121 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 170121 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 170424 7 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155568867 176154 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 176154 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
9948546 16324 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 16324 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
24815434 199696 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593196 199696 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225337 199977 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595151 199977 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815976 199759 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593745 199759 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
798232 200135 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596271 200135 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10615684 18041 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 18041 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 18041 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
44517726 196022 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL560177 196022 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
46225583 200174 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596527 200174 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
1353 1911 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 1911 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 1911 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 1911 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 1911 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9820304 102069 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 102069 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 102069 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
46225334 200046 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595607 200046 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815883 201462 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL604993 201462 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225581 201987 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL608103 201987 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190878 1872 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
6253 1872 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
CHEMBL595759 1872 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
46225584 199675 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593056 199675 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10157556 120235 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 120235 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
3691783 4764 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
CHEMBL103871 4764 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
46225335 200047 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595608 200047 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24849462 199758 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593744 199758 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190877 1871 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
6252 1871 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
CHEMBL605836 1871 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
46225320 201183 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL603443 201183 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9799123 5619 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 5619 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
46225582 201615 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL605831 201615 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225336 200048 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595609 200048 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9952003 5360 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 5360 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
681 1465 72 None -1 15 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 None -1 15 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 None -1 15 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 None -1 15 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 None -1 15 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
228 445 28 None 1 20 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 445 28 None 1 20 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 445 28 None 1 20 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 445 28 None 1 20 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 445 28 None 1 20 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
30699 217704 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
4223 3992 94 None -588 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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 -588 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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 -588 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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 -588 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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 -588 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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
10263487 3069 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105
7683 3069 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
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
124087 1389 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
5329102 194726 86 None - 0 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
1353 1911 93 None -3 83 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 93 None -3 83 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 93 None -3 83 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 93 None -3 83 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 93 None -3 83 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1782 2518 84 None - 22 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 2518 84 None - 22 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 2518 84 None - 22 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 2518 84 None - 22 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 2518 84 None - 22 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
213 3853 55 None -6 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3853 55 None -6 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3853 55 None -6 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3853 55 None -6 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3853 55 None -6 44 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2247 505 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
1613 2348 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
2337 3256 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
2585 803 103 None - 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
3294 2006 111 None -11 45 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -11 45 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -11 45 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -11 45 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -11 45 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
3883 183535 112 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 183535 112 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
135 2532 43 None - 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
2865 4143 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
36811 1454 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 1454 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 1454 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 1454 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 1454 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
1890 2759 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
2286 3183 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2389 3331 118 None -22 67 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -22 67 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -22 67 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -22 67 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -22 67 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
3180 14473 41 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 14473 41 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
5411 204033 89 None - 2 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 204033 89 None - 2 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
135398737 958 93 None -13 89 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -13 89 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -13 89 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -13 89 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -13 89 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
4034 55822 55 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55822 55 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
242 470 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
191 403 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
10831 116963 25 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 116963 25 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
2284 3182 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
1427 2013 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
135398745 2914 112 None -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
5472 205818 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 205818 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 205818 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
135409453 3773 41 None - 2 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
16362 3125 71 None -20 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 71 None -20 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 71 None -20 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 71 None -20 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 71 None -20 30 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3158 56267 27 None - 20 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 - 20 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
212 3806 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
180 401 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3152 188411 103 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188411 103 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
1400 1957 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
21722 17992 31 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 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
14925759 158038 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5290993 194519 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 301 2 1 2 3.0 CC(C)N1C[C@H](NC(=O)N2Cc3ccccc3[C@@H]2C)[C@@H](C)C1 10.1016/j.ejmech.2020.113141
9945233 205092 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 205092 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
25131876 86192 0 None -12 7 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
CHEMBL2312227 86192 0 None -12 7 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
228 445 28 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 445 28 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 445 28 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 445 28 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 445 28 None - 24 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL5277789 193948 0 None -7 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 405 8 2 5 3.7 Oc1cccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.ejmech.2020.113141
CHEMBL5272829 193737 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 320 6 1 3 3.8 CCS[C@H]1CC[C@@H](N(C)CC(=O)Nc2ccc(C)c(C)c2)C1 10.1016/j.ejmech.2020.113141
9857248 205104 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 205104 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
10268039 18016 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126361 18016 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
44315403 205471 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 205471 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL5283608 194220 0 None - 1 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 345 6 0 6 3.0 CCOC(=O)c1nn(-c2ccccc2)cc1CN(C)[C@@H]1CCSC1 10.1016/j.ejmech.2020.113141
164612037 185377 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 185377 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
11392147 18088 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL126754 18088 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
681 1465 72 None -2 39 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 1465 72 None -2 39 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 1465 72 None -2 39 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 1465 72 None -2 39 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 1465 72 None -2 39 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
5025739 169196 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 169196 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
4826074 104104 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL309372 104104 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
5025739 169196 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 169196 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9836662 98153 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL273772 98153 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
45361874 170021 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474209 117374 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL339791 117374 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9835713 18486 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL127226 18486 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 169196 45 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 169196 45 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9858141 117629 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL340099 117629 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9901273 18045 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126510 18045 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
119570 3159 96 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3159 96 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3159 96 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3159 96 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3159 96 None -10 40 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
10336538 1625 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 1625 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 1625 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
5281239 50633 48 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at D4R (unknown origin)Agonist activity at D4R (unknown origin)
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL1575074 50633 48 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at D4R (unknown origin)Agonist activity at D4R (unknown origin)
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL5267339 193520 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 340 5 1 5 3.1 Clc1ccc(-n2cc(CNC[C@@H]3CCCOC3)nn2)c(Cl)c1 10.1016/j.ejmech.2020.113141
681 1465 72 None -2 39 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1465 72 None -2 39 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1465 72 None -2 39 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1465 72 None -2 39 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1465 72 None -2 39 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 1465 72 None -7 39 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
16759175 54994 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1334895 54994 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1616116 54994 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL5289845 194482 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 346 7 3 4 2.7 O=c1cc(CNC[C@@H](CO)Cc2ccsc2)[nH]c2ccc(F)cc12 10.1016/j.ejmech.2020.113141
973 1177 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1177 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1177 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
3303 2244 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 2244 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 2244 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
168294767 193019 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193019 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193019 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9838927 18820 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL127930 18820 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
11255258 18833 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL128040 18833 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 169196 45 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 169196 45 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL5278957 194005 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 363 3 2 2 3.4 CC(C)N1C[C@H](C)[C@H](NC(=O)c2cc3ccc(Br)cc3[nH]2)C1 10.1016/j.ejmech.2020.113141
9966489 18076 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126687 18076 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
16094666 81727 3 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
9945714 18719 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL127752 18719 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
155515982 170010 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 170010 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155568867 176154 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 176154 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
6466372 170062 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3716121 84081 16 None 70 5 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human D4R assessed as [35S] GTPgammaS bindingAgonist activity at human D4R assessed as [35S] GTPgammaS binding
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
CHEMBL2207643 84081 16 None 70 5 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human D4R assessed as [35S] GTPgammaS bindingAgonist activity at human D4R assessed as [35S] GTPgammaS binding
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
9945753 16868 4 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL124927 16868 4 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9857248 205104 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
CHEMBL77708 205104 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
CHEMBL5277325 193932 0 None 35 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at D4R (unknown origin) assessed as beta-arrestin recruitmentAgonist activity at D4R (unknown origin) assessed as beta-arrestin recruitment
ChEMBL 343 7 2 2 3.5 CN(C)[C@@H](CNC(=O)NC[C@H]1Cc2ccccc21)CC1CCCCC1 10.1016/j.ejmech.2020.113141
973 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
9796720 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
CHEMBL77395 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
973 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1177 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
155559617 174884 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174884 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137646281 157806 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157806 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
973 1177 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1177 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1177 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9879627 17056 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
CHEMBL125464 17056 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
4797946 170424 7 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
72901200 119777 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210121
CHEMBL3480577 119777 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210121
72901200 119777 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
CHEMBL3480577 119777 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
228 445 28 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 445 28 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 445 28 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 445 28 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 445 28 None -1 24 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
10225902 18078 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL126698 18078 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
10014924 107271 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 107271 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
9922161 18058 6 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL126595 18058 6 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
10425450 201 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
228 445 28 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 445 28 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 445 28 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 445 28 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 445 28 None - 24 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
4826074 104104 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 104104 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
44381216 120332 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 120332 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
155552185 174061 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174061 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
9815072 18050 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126530 18050 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL5290570 194503 0 None - 1 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 334 4 1 6 2.1 CCOC(=O)c1sc2[nH]cn/c(=N\[C@H]3CCN(CC)C3)c2c1C 10.1016/j.ejmech.2020.113141
3645619 3034 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
975 3034 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
CHEMBL45244 3034 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
9836209 18049 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126529 18049 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
168290235 192968 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192968 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192968 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295528 193031 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193031 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193031 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9945233 205092 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL77563 205092 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
11724450 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 123848 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
9857887 18529 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL127460 18529 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
2 3261 23 None -2 29 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3261 23 None -2 29 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3261 23 None -2 29 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
5281239 50633 48 None - 0 Human 4.1 pEC50 = 4.1 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL1575074 50633 48 None - 0 Human 4.1 pEC50 = 4.1 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
2 3261 23 None -2 29 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 3261 23 None -2 29 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 3261 23 None -2 29 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
9881000 116939 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL338547 116939 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
1588 2325 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
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 10.1021/acs.jmedchem.9b00412
28864 2325 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
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 10.1021/acs.jmedchem.9b00412
43 2325 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
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 10.1021/acs.jmedchem.9b00412
CHEMBL157138 2325 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
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 10.1021/acs.jmedchem.9b00412
DB00589 2325 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
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 10.1021/acs.jmedchem.9b00412
2 3261 23 None -2 29 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 3261 23 None -2 29 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 3261 23 None -2 29 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
681 1465 72 None -2 39 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 1465 72 None -2 39 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 1465 72 None -2 39 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 1465 72 None -2 39 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 1465 72 None -2 39 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
155536720 172187 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
3626837 207315 11 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL93403 207315 11 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
2470 3653 50 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 3653 50 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 3653 50 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 3653 50 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 3653 50 None -20 59 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
14925759 158038 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
3303 2244 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 2244 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 2244 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
10783358 39667 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
CHEMBL147483 39667 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
10406796 100002 10 None -19 5 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL286725 100002 10 None -19 5 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
11738728 18499 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 18499 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
1353 1911 93 None -3 83 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
3559 1911 93 None -3 83 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
86 1911 93 None -3 83 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
CHEMBL54 1911 93 None -3 83 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
DB00502 1911 93 None -3 83 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
9104271 203997 12 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
CHEMBL69584 203997 12 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
10497674 18007 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202219 18007 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126322 18007 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
10570563 18030 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202212 18030 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL126429 18030 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127030612 139330 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 139330 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029391 139348 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 139348 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
118714552 114527 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 114527 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL5288557 194431 0 None - 0 Human 5.0 pIC50 = 5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 535 9 1 5 5.4 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
135512187 34599 5 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
CHEMBL1429613 34599 5 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
168276065 190220 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 190220 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
127030606 139362 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 139362 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
155516494 170121 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 170121 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168296347 192462 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 192462 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
109030343 170860 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170860 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127028185 139336 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 139336 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
16104 161917 19 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
CHEMBL415300 161917 19 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
135398737 958 93 None -13 89 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 958 93 None -13 89 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 958 93 None -13 89 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 958 93 None -13 89 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 958 93 None -13 89 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
10645208 36189 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144494 36189 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373205 36189 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
9868793 96977 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
CHEMBL266393 96977 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
127053218 139478 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 139478 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1016 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
70788951 27155 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 27155 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72737750 114523 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 114523 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168288343 191457 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 191457 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5290330 194496 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 452 5 0 4 3.8 CC(C)(C)N1C=CN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1=O 10.1021/acs.jmedchem.1c00704
10236758 115772 5 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115772 5 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
242 470 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
34 470 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60795 470 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
CHEMBL1112 470 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
DB01238 470 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
9954899 204463 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 204463 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
44363755 121859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL359002 121859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
135398737 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
38 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
722 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
CHEMBL42 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
DB00363 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
168270809 190048 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 190048 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
118719926 115780 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115780 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5275349 193850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 683 8 1 5 7.1 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
CHEMBL5280677 194076 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 478 6 0 4 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)N1C=CN(C2CCCCC2)C(=O)C1 10.1021/acs.jmedchem.1c00704
3191 102858 97 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
127032084 139341 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 139341 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031500 139350 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 139350 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031201 139375 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 139375 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031830 139432 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 139432 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127031513 139474 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 139474 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
72737723 2578 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 2578 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 2578 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
9904205 205850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 205850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 205850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 205850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10594723 17044 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL125455 17044 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
163322330 190700 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 190700 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168287664 191652 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 191652 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
168273063 190285 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 190285 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
16094666 81727 3 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
2726 919 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
135398737 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
38 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
722 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
CHEMBL42 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
DB00363 958 93 None -13 89 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
168293190 192130 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 192130 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5274482 193819 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 442 7 1 4 3.3 CN(CC(=O)NC(C)(C)C)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
1613 2348 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
205 2348 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
3964 2348 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
CHEMBL831 2348 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
DB00408 2348 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
44318454 206009 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 206009 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
10894144 110559 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
CHEMBL325258 110559 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
168277992 190128 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 190128 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
100 3805 58 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -8 55 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
168269421 189962 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 189962 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
20354789 114524 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 114524 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
10026300 167834 17 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 167834 17 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
93601125 139351 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 139351 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
127053198 139372 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 139372 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 139483 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 139483 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
118719926 115780 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115780 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
168282745 191095 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 191095 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
4189 206922 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
135398737 958 93 None -13 89 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
38 958 93 None -13 89 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
722 958 93 None -13 89 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
CHEMBL42 958 93 None -13 89 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
DB00363 958 93 None -13 89 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
168297637 192323 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 192323 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5280979 194091 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 527 8 1 5 5.5 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
21186194 203235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64487 203235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
10739194 116826 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202204 116826 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL337951 116826 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127053215 139424 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 139424 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
72737744 114518 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 114518 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168275962 190619 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 190619 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5278239 193970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 476 9 1 4 3.7 CN(CC(=O)NCc1ccccc1)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
10713599 19402 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202225 19402 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL129324 19402 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
168275089 190496 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 190496 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168279825 190816 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 190816 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168283295 191235 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 191235 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168291848 191872 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 191872 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
137640201 156961 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168290895 191999 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 191999 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
168292124 192025 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 192025 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
44342270 9930 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 9930 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
21186143 203278 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64671 203278 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
135398737 958 93 None -13 89 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
38 958 93 None -13 89 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
722 958 93 None -13 89 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
CHEMBL42 958 93 None -13 89 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
DB00363 958 93 None -13 89 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
9797161 116893 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1204119 116893 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL338337 116893 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
127032086 139322 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 139322 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
72737728 114519 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 114519 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
135398745 2914 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 2914 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 2914 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 2914 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
168292951 192148 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 192148 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
176 398 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
53320010 56664 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in 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 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
127031832 139415 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 139415 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
127030909 139481 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 139481 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
60149678 114517 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 114517 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
42 2063 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
56971 2063 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
CHEMBL8412 2063 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
168279082 190733 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 190733 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
168280464 190736 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 190736 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
45109862 7434 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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
168271806 190519 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 190519 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
10981761 110638 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
CHEMBL325750 110638 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
127031831 139340 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 139340 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10425450 201 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
168280776 191158 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 191158 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
6466372 170062 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168275381 190270 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 190270 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
2812 4779 101 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
168280974 190863 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 190863 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186186 200630 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 200630 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
44336061 108621 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
CHEMBL320597 108621 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
10381889 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 107069 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
10643697 121123 1 None 10 4 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL357448 121123 1 None 10 4 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10450082 102314 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL303519 102314 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
168294958 192404 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 192404 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168289523 191499 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 191499 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
168285068 191583 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 191583 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
127027237 139386 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 139386 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
168275717 190219 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 190219 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5281787 194128 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 553 8 1 5 6.2 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
135398737 958 93 None -13 89 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
38 958 93 None -13 89 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
722 958 93 None -13 89 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
CHEMBL42 958 93 None -13 89 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
DB00363 958 93 None -13 89 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
72737730 114526 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 114526 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
2274 3173 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
155568411 176080 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 176080 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
168281091 191071 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 191071 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186148 202190 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL60957 202190 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10108561 112944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL331077 112944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
155568867 176154 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 176154 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
127028183 139316 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 139316 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127032085 139388 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 139388 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
155513053 169698 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169698 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127027238 139411 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 139411 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL5282604 194165 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 657 7 1 5 6.5 CC(C)(C)NC(=O)Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21 10.1021/acs.jmedchem.1c00704
45482789 198925 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 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 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 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
127027905 139456 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 139456 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
135418440 12068 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 12068 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 12068 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
168296363 192517 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 192517 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10092041 165532 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
CHEMBL424125 165532 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
11730467 11028 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
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 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10688858 18095 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL1202223 18095 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL126793 18095 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
131396 206735 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 206735 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
44304600 203264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64622 203264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
72737767 114520 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 114520 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
21186115 202706 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 202706 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 203258 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 203258 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10666005 17952 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202211 17952 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126032 17952 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
10829708 18044 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202216 18044 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126509 18044 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9799123 5619 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
CHEMBL107742 5619 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
11726532 97026 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL26677 97026 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10688859 18094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202222 18094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL126792 18094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
44363676 40036 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL147897 40036 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373210 40036 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
10572037 121022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL2373204 121022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL356581 121022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
135612922 143701 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
CHEMBL3900329 143701 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
19426635 205593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 205593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
168271259 190515 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 190515 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
163322331 192215 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 192215 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
10688561 116867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202210 116867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL338183 116867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
4797946 170424 7 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3117 207841 103 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
168268918 190007 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 190007 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
135398737 958 93 None -13 89 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
38 958 93 None -13 89 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
722 958 93 None -13 89 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
CHEMBL42 958 93 None -13 89 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
DB00363 958 93 None -13 89 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
127053222 139369 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 139369 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
168270455 190033 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 190033 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
2 3261 23 None -2 29 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
54562 3261 23 None -2 29 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
CHEMBL240773 3261 23 None -2 29 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
135 2532 43 None - 58 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 2532 43 None - 58 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 2532 43 None - 58 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 2532 43 None - 58 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 2532 43 None - 58 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
11071079 110593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
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 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
168294968 192419 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 192419 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
127028505 139333 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 139333 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
4223 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 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 dopamine D4 receptorInhibition of rat dopamine D4 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 dopamine D4 receptorInhibition of rat dopamine D4 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 dopamine D4 receptorInhibition of rat dopamine D4 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 dopamine D4 receptorInhibition of rat dopamine D4 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
168291477 191881 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 191881 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5281830 194132 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 561 9 1 5 6.1 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
19964406 114515 2 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 114515 2 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
53320009 56663 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in 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 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in 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
72737772 114521 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 114521 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
10782111 17887 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202217 17887 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL125910 17887 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
127029388 139339 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 139339 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
45361874 170021 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168277394 190401 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 190401 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
127031516 139309 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 139309 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 139467 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 139467 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
92984956 139480 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 139480 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
46885213 8460 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of dopamine D4 (receptor)Inhibition of dopamine D4 (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 dopamine D4 (receptor)Inhibition of dopamine D4 (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
155530763 171569 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171569 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127031833 139395 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 139395 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
54477 84653 36 None -14 23 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
CHEMBL22242 84653 36 None -14 23 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
72737725 114525 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 114525 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
127029387 139407 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 139407 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
72737734 114522 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 114522 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
10034684 69407 69 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 69407 69 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155562395 175948 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175948 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
54577891 66575 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 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 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 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 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 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
17888044 202923 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 202923 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10832895 120994 7 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
CHEMBL356358 120994 7 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
135398737 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
135398737 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
38 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
722 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
CHEMBL42 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
DB00363 958 93 None -13 89 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
127031518 139399 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 139399 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 139497 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 139497 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
3303 2244 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2244 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2244 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
155511803 169605 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169605 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155536720 172187 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168270563 189950 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 189950 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
11035765 9888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
CHEMBL114280 9888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
11793971 17966 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202202 17966 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126126 17966 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
109030515 175985 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175985 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168292271 191889 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 191889 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
168295019 192499 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 192499 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
10668173 19443 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202206 19443 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL129556 19443 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
127053214 139349 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 139349 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
155515982 170010 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 170010 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127031829 139428 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 139428 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 139462 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 139462 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
127029386 139397 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 139397 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
44363656 35475 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL143835 35475 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373208 35475 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
71717830 85983 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 85983 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
168275515 190505 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 190505 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10851217 118525 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL341497 118525 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
44304314 102692 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL304692 102692 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
155559617 174884 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174884 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
135514603 204114 14 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL70319 204114 14 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
3303 2244 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 2244 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 2244 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5615 3899 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 3899 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 3899 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
1353 1911 93 None -3 83 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 1911 93 None -3 83 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 1911 93 None -3 83 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 1911 93 None -3 83 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 1911 93 None -3 83 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9901894 163416 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202220 163416 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL419610 163416 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
11301655 200 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 200 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 200 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
127031515 139434 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 139434 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5274672 193825 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 527 7 1 5 5.7 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.1c00704
135620651 144508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
CHEMBL3906995 144508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
135398737 958 93 None -13 89 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 958 93 None -13 89 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 958 93 None -13 89 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 958 93 None -13 89 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 958 93 None -13 89 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
127053220 139367 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 139367 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
11005810 10466 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
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 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL5278254 193971 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 497 6 1 5 3.0 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NC(C)(C)C)C1 10.1021/acs.jmedchem.1c00704
51003551 56670 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in 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 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in 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
127031515 139434 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 139434 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
1353 1911 93 None -3 83 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1911 93 None -3 83 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1911 93 None -3 83 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1911 93 None -3 83 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1911 93 None -3 83 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10803754 18107 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203257 18107 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126847 18107 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
21186102 100777 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL292943 100777 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10049758 204645 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL73589 204645 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
137640201 156961 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168287735 191804 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 191804 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5266395 193478 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 486 7 0 4 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)N1C=CN(Cc2ccccc2)C(=O)C1 10.1021/acs.jmedchem.1c00704
127031519 139323 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 139323 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 139331 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 139331 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127032383 139403 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 139403 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
135398737 958 93 None -13 89 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 958 93 None -13 89 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 958 93 None -13 89 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 958 93 None -13 89 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 958 93 None -13 89 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
1212 1662 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
127032082 139317 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 139317 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
21186124 102212 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302904 102212 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 203258 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 203258 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10617133 17999 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202214 17999 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126269 17999 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 102069 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 102069 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 102069 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
1353 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10236758 115772 5 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115772 5 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
1353 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
3559 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
86 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
CHEMBL54 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
DB00502 1911 93 None -3 83 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
10385977 97331 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
CHEMBL26929 97331 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
CHEMBL5270832 193655 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 523 7 1 5 3.5 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NC2CCCCC2)C1 10.1021/acs.jmedchem.1c00704
2247 505 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
127031508 139381 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 139381 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
155552185 174061 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174061 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127053217 139318 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 139318 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
45278882 7452 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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
168274850 190155 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 190155 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
168274755 190642 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 190642 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
127032083 139447 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 139447 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
72198754 90880 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 90880 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
10905740 110670 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL325945 110670 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL5266508 193484 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 497 6 2 5 2.1 CC(C)(C)NC(=O)C1C(=O)NCCN1C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
10615990 117305 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202209 117305 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL339674 117305 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127053219 139464 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 139464 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL5269858 193612 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 523 7 2 5 2.7 O=C1NCCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C1C(=O)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
15840855 102089 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 102089 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186186 200630 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 200630 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186138 202698 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61657 202698 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186115 202706 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 202706 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9797162 78341 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2092961 78341 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2109988 78341 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
10501113 36547 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL144811 36547 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL5273880 193783 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 501 7 1 5 5.0 CC(C)(C)NC(=O)Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21 10.1021/acs.jmedchem.1c00704
10762827 121927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL2373207 121927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL359051 121927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
10411988 21410 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 21410 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
11113605 10507 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
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 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10496095 116830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202224 116830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL337983 116830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
155536815 172207 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 172207 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
10739483 36621 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144868 36621 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373206 36621 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL5268231 193553 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 468 8 1 4 3.8 CN(CC(=O)NC1CCCCC1)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
127028181 139449 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 139449 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10885636 111016 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
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 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
155563301 175250 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 175250 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
5615 3899 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 3899 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 3899 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
21186098 100543 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL291380 100543 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
21186192 100603 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL291824 100603 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10615684 18041 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 18041 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 18041 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
9967140 18067 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202215 18067 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126633 18067 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127032384 139376 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 139376 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10568183 17978 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202221 17978 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL126182 17978 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
44363675 119253 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL2373209 119253 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL343620 119253 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
168286314 191659 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 191659 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5283891 194233 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 531 8 2 5 2.5 O=C1NCCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C1C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
15840855 102089 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 102089 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
17888044 202923 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 202923 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10808230 18061 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202205 18061 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126604 18061 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 102069 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 102069 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 102069 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
10761040 118470 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL1202213 118470 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL341310 118470 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
14925759 158038 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5278601 193987 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 691 9 1 5 6.9 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
CHEMBL5273430 193763 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 531 8 1 5 3.4 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NCc2ccccc2)C1 10.1021/acs.jmedchem.1c00704
127029389 139443 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 139443 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
3303 2244 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2244 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2244 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
3198 205513 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10948527 111355 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
CHEMBL326962 111355 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
135492584 11333 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 11333 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 11333 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
135481864 12350 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 12350 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 12350 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
168284020 191253 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 191253 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10780076 18005 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203260 18005 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126318 18005 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
127031497 139491 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 139491 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
4452 2762 19 None -7 19 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
983 2762 19 None -7 19 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
CHEMBL20734 2762 19 None -7 19 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
45278805 7450 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 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
164612037 185377 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 185377 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192968 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192968 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192968 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 193019 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193019 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193019 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 193031 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193031 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193031 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4452 2762 19 None -7 19 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
983 2762 19 None -7 19 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
CHEMBL20734 2762 19 None -7 19 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
9849682 94952 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 94952 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
10162564 12540 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 12540 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 12540 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
3251 4072 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
5684 4072 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
80 4072 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
CHEMBL31354 4072 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
11724450 123848 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123848 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123848 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
17955460 176775 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 176775 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
2030 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
5311377 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
CHEMBL251541 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
2030 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 3672 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
44447073 94550 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 94550 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
11729231 49610 0 None 1584 4 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL156599 49610 0 None 1584 4 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
11131951 49921 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
CHEMBL156845 49921 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
4257 78255 30 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
CHEMBL2106650 78255 30 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
3504099 92160 6 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420894 92160 6 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
10948748 50456 0 None 676 3 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
CHEMBL157322 50456 0 None 676 3 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
3626837 207315 11 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL93403 207315 11 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
3626837 207315 11 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL93403 207315 11 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
16363 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
312 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
9215 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
CHEMBL297302 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
DB12867 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
2470 3653 50 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 3653 50 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 3653 50 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 3653 50 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 3653 50 None -20 59 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
72901200 119777 25 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
CHEMBL3480577 119777 25 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
11090403 119544 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL345848 119544 0 None 2 3 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
9977532 111191 1 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 111191 1 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
11574902 78450 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL211164 78450 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
155515982 170010 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 170010 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11574902 78450 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
CHEMBL211164 78450 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
11036114 50521 0 None 134 3 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
CHEMBL157388 50521 0 None 134 3 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
17449900 139542 13 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139542 13 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
10733406 19441 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL129534 19441 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10733406 19441 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL129534 19441 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
10546540 207237 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL92859 207237 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
11583188 139282 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL379125 139282 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
2470 3653 50 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
3300 3653 50 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
5265 3653 50 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
99 3653 50 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
CHEMBL267930 3653 50 None -20 59 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
5041 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
981 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
CHEMBL4096543 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
11583188 139282 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 139282 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
5041 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
981 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
CHEMBL4096543 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
5041 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
981 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
CHEMBL4096543 3294 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
49788939 18259 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270323 18259 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
10780510 19497 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
CHEMBL129927 19497 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
10780510 19497 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
CHEMBL129927 19497 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
44400585 68655 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68655 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
21219157 98900 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
CHEMBL279247 98900 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
21219157 98900 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL279247 98900 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
3716121 84081 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
CHEMBL2207643 84081 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
3716121 84081 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207643 84081 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
168287284 192935 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5198170 192935 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222300 192935 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
3303 2244 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
5311200 2244 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
CHEMBL267014 2244 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
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 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
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 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
44412482 78159 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
CHEMBL210404 78159 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
44412482 78159 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210404 78159 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
2470 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
3300 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
5265 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
99 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
CHEMBL267930 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
44436598 149295 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL394473 149295 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
2470 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
3300 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
5265 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
99 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL267930 3653 50 None -20 59 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
10660814 18872 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL128232 18872 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10667579 207386 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
CHEMBL93832 207386 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
10660814 18872 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL128232 18872 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
119570 3159 96 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3159 96 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3159 96 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3159 96 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3159 96 None -10 40 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL5285358 194294 0 None 7413 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 4 2 4 3.3 O/N=C/c1c(CN2CCN(c3ccccc3)CC2)[nH]c2ccccc12 10.1016/j.ejmech.2020.113141
6603897 2247 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
978 2247 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL60518 2247 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
168268758 192765 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 192765 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 192765 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
10708280 18950 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128647 18950 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10450892 21871 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
CHEMBL131997 21871 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
9995904 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
CHEMBL140099 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
9995904 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
9995904 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL140099 31219 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
44400674 125189 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 125189 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10708280 18950 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128647 18950 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10450892 21871 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
CHEMBL131997 21871 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
10315310 22883 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132884 22883 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10315310 22883 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132884 22883 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11655570 79726 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
CHEMBL211590 79726 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
32224 206905 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
CHEMBL90882 206905 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
32224 206905 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL90882 206905 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
3303 2244 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
5311200 2244 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
CHEMBL267014 2244 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
44326285 111542 0 None 2 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL327984 111542 0 None 2 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
9888765 189618 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
CHEMBL514848 189618 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
155552185 174061 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174061 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155559617 174884 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 174884 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10522613 206958 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91229 206958 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
44419065 84323 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL221600 84323 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
11983282 138943 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138943 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
9950165 206949 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91162 206949 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
44400519 133129 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 133129 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
168268758 192765 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 192765 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 192765 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
9977022 192891 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5189614 192891 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222031 192891 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
10783358 39667 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
CHEMBL147483 39667 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
11676195 195148 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 195148 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
44400626 70402 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70402 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10547607 206946 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL91155 206946 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL5272162 193711 0 None 3162 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 321 4 2 3 3.0 OCc1[nH]c2ccccc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
168285556 192917 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
11057969 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
CHEMBL141845 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
11057969 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL141845 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10669042 108144 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
CHEMBL319597 108144 0 None -2 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
168268850 192784 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5179930 192784 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221350 192784 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
11057969 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL141845 33271 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
25072633 159221 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 159221 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
168268839 192781 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5177462 192781 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221334 192781 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
792584 92152 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420779 92152 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
3303 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
5311200 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
CHEMBL267014 2244 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
41532205 78277 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210717 78277 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
2653640 66219 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 66219 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
10450375 99491 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
CHEMBL28321 99491 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
41532205 78277 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
CHEMBL210717 78277 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
10643588 207423 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94023 207423 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
71456045 84073 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 84073 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
49782398 17452 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1257688 17452 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
122191607 123722 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 123722 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
25093832 155880 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155880 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
1353 1911 93 None -3 83 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
3559 1911 93 None -3 83 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
86 1911 93 None -3 83 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
CHEMBL54 1911 93 None -3 83 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
DB00502 1911 93 None -3 83 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
10594764 111773 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328739 111773 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
983 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
CHEMBL20734 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
CHEMBL5278853 194000 0 None 3311 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1[nH]c2ccccc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
44340097 9440 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9440 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
102505294 192999 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 192999 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 192999 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
71454295 84079 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 84079 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10638052 20092 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130402 20092 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
60165418 75349 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037521 75349 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
10734727 19462 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL129757 19462 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
9977532 111191 1 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 111191 1 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10783874 207047 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
CHEMBL91669 207047 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
10734727 19462 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL129757 19462 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
60165418 75349 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL2037521 75349 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
11697270 77310 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
CHEMBL208274 77310 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
10522614 207017 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91498 207017 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
983 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
CHEMBL20734 2762 19 None -7 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
168274496 192812 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175054 192812 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221490 192812 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
12765116 206519 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL88464 206519 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
3303 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
5311200 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
CHEMBL267014 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
3303 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
5311200 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
CHEMBL267014 2244 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
44400553 70779 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70779 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
49788941 18274 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
CHEMBL1270423 18274 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
11689612 79839 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
CHEMBL212160 79839 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
10247720 13054 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 13054 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 13054 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10447709 21286 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131357 21286 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
76325150 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10248715 167877 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
CHEMBL431095 167877 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
10447709 21286 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
CHEMBL131357 21286 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
76325150 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 106422 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10236758 115772 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL3354065 115772 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
168268756 192764 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 192764 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 192764 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10236758 115772 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115772 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
11516033 139118 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
CHEMBL378680 139118 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
122180954 121769 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589575 121769 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11575799 78129 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL210341 78129 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
11661609 79693 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
CHEMBL211539 79693 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
9951735 205255 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
CHEMBL78923 205255 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
10594242 206748 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL90005 206748 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014692 204921 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL7617 204921 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
1353 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10314824 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
CHEMBL143761 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
10314824 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
44412182 77266 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL208018 77266 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
10403608 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210405 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44412182 77266 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
CHEMBL208018 77266 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
10403608 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210405 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
10403608 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL210405 78160 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
10314824 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL143761 35380 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
1353 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
3559 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
86 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
CHEMBL54 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
DB00502 1911 93 None -3 83 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
102505294 192999 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 192999 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 192999 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
168289100 192951 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5191299 192951 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222419 192951 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
10732925 115217 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL334545 115217 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
90644061 112033 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 112033 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
10666315 96589 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL263162 96589 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
10809899 206745 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL89971 206745 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
511482 97252 6 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268799 97252 6 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10570479 112274 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL329106 112274 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10732925 115217 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
CHEMBL334545 115217 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
10406796 100002 10 None -19 5 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL286725 100002 10 None -19 5 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
9805944 56227 37 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 56227 37 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
90644061 112033 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 112033 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
9797495 69004 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
CHEMBL1923292 69004 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
44340227 110641 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110641 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10619737 202399 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL61079 202399 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
681 1465 72 None -2 39 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1465 72 None -2 39 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1465 72 None -2 39 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1465 72 None -2 39 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1465 72 None -2 39 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
10494394 168549 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
CHEMBL435598 168549 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
137651936 157392 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 157392 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
21219176 96291 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL26120 96291 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10619737 202399 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
CHEMBL61079 202399 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
45273045 196376 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 196376 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10427977 54465 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160952 54465 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
10494394 168549 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL435598 168549 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
10088259 101913 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 101913 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
10427977 54465 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL160952 54465 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
137640201 156961 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156961 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
9905249 99902 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL28607 99902 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10762432 207413 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
CHEMBL93969 207413 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
10740483 207131 0 None 3 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL92192 207131 0 None 3 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
44454709 97518 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL270406 97518 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
10450375 99491 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL28321 99491 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
16094698 137868 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 137868 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
25256816 181608 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 181608 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10450375 99491 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28321 99491 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
10406796 100002 10 None -19 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL286725 100002 10 None -19 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
25072002 156114 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 156114 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
11696910 77747 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
CHEMBL209034 77747 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
11631892 78111 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
CHEMBL210283 78111 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
10359942 102936 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL306265 102936 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
168294165 193012 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5209074 193012 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222773 193012 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
137645938 157583 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 157583 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
9863333 204365 0 None 1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL71724 204365 0 None 1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
2470 3653 50 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
3300 3653 50 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
5265 3653 50 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
99 3653 50 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
CHEMBL267930 3653 50 None -20 59 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
10615787 116763 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL337627 116763 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
16094666 81727 3 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10498094 32318 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
CHEMBL141035 32318 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
122181333 121874 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 121874 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11516033 139118 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL378680 139118 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
1353 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
10314060 168600 0 None 72 7 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 168600 0 None 72 7 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
1353 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
3559 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
86 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
CHEMBL54 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
DB00502 1911 93 None -3 83 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
168285556 192917 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 192917 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 192917 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
9883587 111555 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL328054 111555 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
44394743 123101 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL361035 123101 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
10595908 205258 1 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL78933 205258 1 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
10567839 207033 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91585 207033 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
10716772 207286 0 None 3 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL93198 207286 0 None 3 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
9883587 111555 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL328054 111555 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
12765746 102280 4 None -6 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 102280 4 None -6 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
11725531 54054 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/j.ejmech.2020.113141
CHEMBL160626 54054 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/j.ejmech.2020.113141
CHEMBL5280364 194065 0 None 10000 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 5 1 4 3.8 CCOC(=O)c1[nH]c2ccc(F)cc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
11301655 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
8441 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
CHEMBL127257 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
10473554 72947 0 None 2089 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 357 5 1 4 3.5 Clc1ccc(OCC2CN(Cc3c[nH]c4ncccc34)CCO2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL2005767 72947 0 None 2089 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 357 5 1 4 3.5 Clc1ccc(OCC2CN(Cc3c[nH]c4ncccc34)CCO2)cc1 10.1016/j.ejmech.2020.113141
57403525 70154 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
57403525 70154 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 70154 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940402 70154 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
44394743 123101 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL361035 123101 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
25093832 155880 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155880 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137660837 159080 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 159080 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
71456046 84075 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 84075 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44381216 120332 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 120332 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
44371997 49930 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
CHEMBL156851 49930 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
11725531 54054 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 54054 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
11301655 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
11301655 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
8441 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL127257 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
49788869 18224 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
CHEMBL1270121 18224 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
127049060 140775 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 140775 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
76321554 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
9954003 71700 24 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 71700 24 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
1353 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
3559 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
86 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
CHEMBL54 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
DB00502 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
76321554 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 106403 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
44340084 9088 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9088 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10618875 104222 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL309901 104222 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
9104271 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL69584 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44454711 97519 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL270408 97519 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
511482 97252 6 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL268799 97252 6 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
9104271 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL69584 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9104271 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL69584 203997 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
10336039 119235 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
CHEMBL343466 119235 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
127049060 140775 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 140775 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
11682812 78209 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
CHEMBL210551 78209 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
11581237 138958 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
CHEMBL378515 138958 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
44376876 120172 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351611 120172 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
155536720 172187 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
10690200 207129 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL92189 207129 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
44323978 105283 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
CHEMBL311539 105283 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
76316875 85887 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298810 85887 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
24882561 95341 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL256637 95341 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
155527714 171296 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4460743 171296 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
11726532 97026 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26677 97026 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
44376569 57441 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 57441 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44376918 120012 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL350160 120012 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
42266988 18245 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270227 18245 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
168268695 192774 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5170580 192774 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5221253 192774 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
21462964 48185 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL155207 48185 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
11792163 42076 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL149596 42076 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
44454735 95317 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL256492 95317 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
10643697 121123 1 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL357448 121123 1 None 10 4 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
44209472 70172 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 70172 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209472 70172 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940420 70172 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
2 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
2653640 66219 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 66219 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
2 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
2 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3261 23 None -2 29 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
4797946 170424 7 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10837488 112652 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL330318 112652 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22065971 121097 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
CHEMBL357182 121097 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
25256814 181612 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 181612 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
71457844 84076 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 84076 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
56652776 193008 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5205590 193008 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222747 193008 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788867 18206 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
CHEMBL1270013 18206 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
137642607 158518 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 158518 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10588194 18920 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128524 18920 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44336061 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
CHEMBL320597 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
10520941 205112 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
CHEMBL77744 205112 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
9948584 207379 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93779 207379 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44273720 75195 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20367 75195 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
9801098 5401 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
CHEMBL107151 5401 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
44335908 5989 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108011 5989 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
44336075 4909 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104579 4909 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
9948546 16324 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 16324 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
44374827 119497 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL345438 119497 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL5277789 193948 0 None -7 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 405 8 2 5 3.7 Oc1cccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.ejmech.2020.113141
164627977 186433 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 186433 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
1353 1911 93 None -4 83 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 1911 93 None -4 83 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 1911 93 None -4 83 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 1911 93 None -4 83 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 1911 93 None -4 83 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
52940985 17586 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258155 17586 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
137651322 157475 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 157475 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
122180956 121771 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 121771 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
2389 3331 118 None -22 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 3331 118 None -22 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 3331 118 None -22 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 3331 118 None -22 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 3331 118 None -22 67 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
9887537 84345 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL221692 84345 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL4751170 84345 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
11725909 204268 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71216 204268 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
1353 1911 93 None -3 83 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 1911 93 None -3 83 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 1911 93 None -3 83 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 1911 93 None -3 83 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 1911 93 None -3 83 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9907461 134242 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL37169 134242 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
9903877 200326 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
CHEMBL59752 200326 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
135398737 958 93 None -13 89 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
38 958 93 None -13 89 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
722 958 93 None -13 89 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
CHEMBL42 958 93 None -13 89 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
DB00363 958 93 None -13 89 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
127029388 139339 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 139339 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
164938016 192969 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5200816 192969 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222506 192969 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
164627977 186433 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 186433 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
127031516 139309 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 139309 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 139467 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 139467 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1353 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9902382 42725 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150173 42725 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
127029387 139407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 139407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
10590285 20054 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL130370 20054 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
12997400 101004 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL294394 101004 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
11726130 56476 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
CHEMBL163239 56476 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
44273884 77058 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20729 77058 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
9820048 203643 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
CHEMBL67222 203643 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
10811059 205614 5 None 23 4 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81649 205614 5 None 23 4 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
135398737 958 93 None -13 89 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -13 89 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -13 89 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -13 89 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -13 89 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2914 112 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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 -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 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
2389 3331 118 None -22 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3331 118 None -22 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3331 118 None -22 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3331 118 None -22 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3331 118 None -22 67 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
44403219 71904 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
CHEMBL197162 71904 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
242 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
72205043 91944 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414354 91944 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
118719927 115781 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354074 115781 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
60165681 75356 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037528 75356 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
25139335 184318 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
CHEMBL484203 184318 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
57402366 69315 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 69315 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
72545239 93128 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 93128 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44436621 91031 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL239733 91031 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
242 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
11245414 5119 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105661 5119 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
154703647 176365 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4450429 176365 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 176365 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
242 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 470 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
13014683 97343 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL269396 97343 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1687 104409 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL310310 104409 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL540034 104409 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
242 470 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
33630 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
127046951 139902 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139902 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
11360927 4971 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
CHEMBL104844 4971 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
145980271 166492 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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 -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
46216855 200378 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 200378 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 200408 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 200408 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231848 200538 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 200538 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231845 200733 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 200733 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46232066 201256 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 201256 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
11439190 201305 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 201305 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231995 201534 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 201534 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231927 201536 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 201536 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
164627027 186427 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
CHEMBL4876260 186427 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
863787 66291 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 66291 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
168276065 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
168276065 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5174753 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
44395711 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456430 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537183 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395711 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456430 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL537183 174899 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL5085974 215004 0 None -123 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44309775 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
CHEMBL304605 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
44309775 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL304605 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
44309775 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
CHEMBL304605 102678 0 None -288 8 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
72737772 114521 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 114521 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
168276065 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5174753 190220 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
56664948 66433 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813587 66433 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851962 66433 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44431482 88036 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234473 88036 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
1353 1911 93 None -3 83 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
3559 1911 93 None -3 83 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
86 1911 93 None -3 83 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
CHEMBL54 1911 93 None -3 83 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
DB00502 1911 93 None -3 83 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
10512444 24910 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134571 24910 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
155536631 172220 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 172220 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
155536631 172220 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 172220 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
42625295 56251 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627321 56251 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
164612428 185163 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
CHEMBL4857166 185163 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
168296347 192462 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 192462 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
154725484 176465 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 176465 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 176465 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
168280974 190863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5184607 190863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
10983150 102988 0 None -18 5 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL306672 102988 0 None -18 5 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
763625 92148 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420775 92148 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
60165412 75359 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037530 75359 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
130431351 173171 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4521947 173171 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
168280974 190863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5184607 190863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
23288790 203964 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL69385 203964 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9885219 56275 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162873 56275 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
127031833 139395 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 139395 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
135506137 11334 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179504 11334 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80655 11334 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10065188 101604 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 101604 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
11408148 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
CHEMBL366904 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
11408148 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
164623294 185823 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
CHEMBL4867331 185823 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
11408148 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL366904 128720 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
72737725 114525 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 114525 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
4350931 169313 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 169313 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
44336154 5440 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
CHEMBL107384 5440 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
4350931 169313 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 169313 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
21302490 112805 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 112805 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 112805 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
188249 39653 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL147463 39653 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL2022280 39653 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
10363821 39037 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146856 39037 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
10807035 206732 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL89921 206732 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10615437 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL25938 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
15467370 102318 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL303538 102318 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
10807035 206732 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL89921 206732 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
289 242 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 242 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 242 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
72164301 92159 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420893 92159 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44330553 168199 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL433376 168199 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10590285 20054 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
CHEMBL130370 20054 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
44335909 111339 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326863 111339 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
10926404 46860 9 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
CHEMBL154050 46860 9 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
44335853 4859 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104321 4859 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 1911 93 None -3 83 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
10782946 15573 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL122049 15573 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
9906978 42711 2 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL150161 42711 2 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
2435 3590 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 3590 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 3590 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 3590 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 3590 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
145969934 165045 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 165045 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11504230 78217 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
CHEMBL210567 78217 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
11393666 192986 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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 -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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 -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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
CHEMBL4435399 213924 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None O=[N+]([O-])c1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
16725912 85729 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
16725912 85729 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL228972 85729 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL228972 85729 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44431489 88271 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234825 88271 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
53364155 63844 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803026 63844 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
137632761 156574 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 156574 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137640203 156962 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 156962 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
10615437 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL25938 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
71733935 90983 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2396663 90983 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10615437 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL25938 95941 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
9865446 124051 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL36313 124051 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10479188 202873 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62602 202873 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
9949531 206609 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL89037 206609 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44369020 119459 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
CHEMBL345111 119459 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
11558055 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
11558055 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL1204122 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
11558055 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 73152 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11772112 168816 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 168816 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
44278427 99342 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL282323 99342 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
127031518 139399 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 139399 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 139497 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 139497 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
11849266 81069 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 81069 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
44370047 119676 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347155 119676 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
13091268 78224 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 78224 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10378389 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10378389 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 203245 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10497193 204937 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76355 204937 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10738530 205035 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77017 205035 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10790517 207612 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL95096 207612 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
6603867 101994 17 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL301559 101994 17 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
57345618 70459 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946126 70459 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
92984956 139480 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 139480 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11164276 79752 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 79752 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11154555 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL3085826 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 800 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
10830557 31301 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL140165 31301 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
44436600 91802 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 91802 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
71734126 91054 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397391 91054 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
44372312 53785 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL160396 53785 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
72737734 114522 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 114522 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
155536815 172207 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 172207 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
133633 2241 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 2241 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 2241 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
44438201 93607 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246637 93607 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25139329 187103 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL491466 187103 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
2779264 111342 38 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL326877 111342 38 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
134151428 154552 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3978642 154552 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991094 154552 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
17755999 142885 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 142885 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
3117 207841 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44304644 203251 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
CHEMBL64566 203251 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
10436285 101952 0 None -954 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 101952 0 None -954 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
10301202 13502 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1193508 13502 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL544925 13502 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
11211058 80334 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 80334 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44393737 65761 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 65761 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
154703824 176626 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4456007 176626 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 176626 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
145967904 165097 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 165097 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11812838 203885 0 None -47 5 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL68860 203885 0 None -47 5 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154726046 176311 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442408 176311 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595266 176311 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
168282745 191095 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5187721 191095 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168288343 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5193214 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
136094867 40569 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148353 40569 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
155511803 169605 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 169605 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
164622586 185536 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4862839 185536 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
168288343 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5193214 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
168288343 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 191457 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
168282745 191095 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5187721 191095 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
10378389 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL134807 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL64553 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
10378389 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL134807 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL64553 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
10378389 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL134807 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL64553 203245 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
44431462 88069 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234640 88069 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10411988 21410 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 21410 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
122334 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
970 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
CHEMBL27441 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
122334 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
970 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
CHEMBL27441 322 23 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
22727358 13224 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191251 13224 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL542324 13224 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
127049059 140813 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 140813 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
85658088 165003 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 165003 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
127049059 140813 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 140813 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
72205222 91948 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414358 91948 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
162669562 182702 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 182702 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44431467 154432 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL398990 154432 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
44438229 154899 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL400826 154899 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
142590728 181522 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4765081 181522 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
10618211 78603 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112285 78603 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44300865 201995 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 201995 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
10424172 13788 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195497 13788 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL554670 13788 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
44323894 168100 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL432762 168100 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10619612 172680 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL450021 172680 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
44323894 168100 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL432762 168100 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10617381 189686 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 189686 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44454710 155666 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL404888 155666 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
9859861 168080 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 168080 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
44335973 5034 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105172 5034 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335893 108605 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL320515 108605 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335746 5699 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107804 5699 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335829 108596 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL320440 108596 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335828 163457 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419916 163457 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
155561779 175765 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4583596 175765 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
44374863 120207 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351989 120207 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
90644057 112032 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 112032 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
13091268 78224 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL210578 78224 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
53364226 63846 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803028 63846 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363201 63855 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803054 63855 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
44300865 201995 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL60815 201995 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
44436599 91801 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241211 91801 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
44222483 196251 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 196251 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
45271653 195235 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL550920 195235 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
10251080 13959 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196692 13959 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL557829 13959 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
13091268 78224 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 78224 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10617381 189686 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 189686 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11792373 119822 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL348435 119822 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
127053214 139349 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 139349 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
76282192 193033 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5207313 193033 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222877 193033 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
9949601 100053 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL287078 100053 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
44264644 204743 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7442 204743 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
155563301 175250 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 175250 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44273927 75545 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20444 75545 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273924 75907 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20493 75907 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9863108 78076 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21008 78076 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
90644057 112032 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 112032 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
1353 1911 93 None -3 83 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
3559 1911 93 None -3 83 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
86 1911 93 None -3 83 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
CHEMBL54 1911 93 None -3 83 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
DB00502 1911 93 None -3 83 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
10382581 101298 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 101298 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
90644067 112020 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 112020 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
11724853 97020 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
CHEMBL266723 97020 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
12066264 14415 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12004 14415 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
11849182 79869 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 79869 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
49782836 17552 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1258036 17552 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
49782837 17585 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1258154 17585 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11706497 78177 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 78177 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
44436605 149063 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 149063 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
11517928 77103 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL207543 77103 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
45269161 196335 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL562384 196335 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44381424 59071 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169562 59071 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
162669562 182702 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 182702 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
168270809 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
CHEMBL5172055 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
164623862 186005 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 186005 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
168270809 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
10826290 205483 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
CHEMBL80552 205483 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
21219173 93455 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24603 93455 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44319361 205720 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 205720 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
71717830 85983 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 85983 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
168280776 191158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5188602 191158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
44374637 55265 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161811 55265 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
168270809 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
CHEMBL5172055 190048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
164623862 186005 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 186005 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
168280776 191158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5188602 191158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
44591089 189482 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL513776 189482 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
57390695 70467 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946257 70467 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57390695 70467 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946257 70467 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
127052778 140845 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 140845 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
164623991 185537 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185537 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9980998 31035 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 31035 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 31035 0 None -1148 8 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
11203294 75831 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75831 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
3695490 100595 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29179 100595 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
57345619 70464 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946253 70464 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
127050699 140872 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 140872 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 140872 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
164623991 185537 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185537 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
25141533 92167 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL242218 92167 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
9888494 98171 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 98171 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
73213196 104460 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104460 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
127052778 140845 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 140845 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
11203294 75831 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 75831 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL5086258 215019 0 None -199 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor by radioligand binding assayBinding affinity to human D4 receptor by radioligand binding assay
ChEMBL None None None Cc1cc(I)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
136094687 13438 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL1192972 13438 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL544296 13438 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
15467373 101854 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL300553 101854 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
44273715 73123 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20114 73123 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273877 98734 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277937 98734 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
44273553 98788 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL278288 98788 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
134155461 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44273552 79930 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21252 79930 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9827938 11771 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11771 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11771 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
57402951 70468 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946258 70468 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57402951 70468 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946258 70468 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5071238 214253 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CC(O)CCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
CHEMBL5070377 214235 0 None -251 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11335419 67100 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 67100 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
134155461 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 154487 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44376921 57325 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165113 57325 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
49783415 17678 0 None -524 12 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17678 0 None -524 12 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
134133968 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
10476504 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL142020 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
11663604 83173 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
CHEMBL218351 83173 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
155539605 172845 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 172845 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
46912548 14393 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173288 14393 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200271 14393 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44438210 93371 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245615 93371 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
134133968 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 154523 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
42625293 56249 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 56249 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
44330292 4508 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL102162 4508 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
44330515 208398 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99654 208398 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
154706711 176515 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4439535 176515 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596930 176515 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
10760813 164089 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL420954 164089 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
44264623 205013 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7686 205013 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44336138 4873 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104380 4873 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
90644067 112020 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 112020 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
90644060 112031 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
CHEMBL3289644 112031 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
135398737 958 93 None -13 89 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
38 958 93 None -13 89 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
722 958 93 None -13 89 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
CHEMBL42 958 93 None -13 89 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
DB00363 958 93 None -13 89 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
53363110 63851 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803050 63851 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
24936042 157589 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157589 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
6603820 95774 19 None -1 13 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 95774 19 None -1 13 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
11428416 5295 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106599 5295 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11406804 164462 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL421403 164462 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
127029386 139397 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 139397 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11772767 80002 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 80002 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
164628817 186277 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 186277 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
11849775 166196 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 166196 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
44340376 110646 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110646 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10476504 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44403214 72493 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL198993 72493 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
44393393 123673 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
CHEMBL362101 123673 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
44381147 58729 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168544 58729 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
55445 98548 18 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
CHEMBL276500 98548 18 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
154724369 176689 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4584372 176689 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598389 176689 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
127031829 139428 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 139428 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 139462 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 139462 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL5290570 194503 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 334 4 1 6 2.1 CCOC(=O)c1sc2[nH]cn/c(=N\[C@H]3CCN(CC)C3)c2c1C 10.1016/j.ejmech.2020.113141
11370781 79871 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 79871 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
25071066 111774 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 111774 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
56837634 69306 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 69306 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709172 113419 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318844 113419 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
137655029 158946 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4095881 158946 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
9995378 5473 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL107529 5473 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
276 3513 50 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
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 -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
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 -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
10476504 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 33487 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
122189388 123243 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 123243 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
119570 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
11077918 206594 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
CHEMBL88937 206594 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
11077918 206594 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
CHEMBL88937 206594 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
10021692 146382 19 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL392158 146382 19 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
11708363 71902 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL197159 71902 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
76336022 106379 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 106379 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 106379 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
136094866 40959 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148694 40959 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
168285068 191583 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5195130 191583 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
127051516 140857 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 140857 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
56678599 66422 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813586 66422 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851900 66422 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
154725001 176647 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4525624 176647 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 176647 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
145980875 166707 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4282702 166707 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
127051516 140857 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 140857 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
71062646 149543 0 None -218 12 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 149543 0 None -218 12 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
154727713 176364 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514586 176364 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 176364 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
168287664 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
154703922 176289 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4590211 176289 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 176289 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44335972 109747 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL323022 109747 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44355355 24181 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL133938 24181 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
11849816 78079 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 78079 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
168287664 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5196102 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
5249956 73395 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73395 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
163322330 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5182191 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
168287664 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5196102 191652 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164611932 185202 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 185202 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
168273063 190285 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 190285 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
11028157 202721 0 None -128 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
CHEMBL61789 202721 0 None -128 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
10183626 13048 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190010 13048 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539999 13048 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
127052466 140786 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 140786 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
163322330 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5182191 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
163322330 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 190700 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
145968810 165038 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 165038 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
56658006 66370 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813588 66370 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851643 66370 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44436300 148836 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL394110 148836 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
44438206 147209 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL392823 147209 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
44336046 4805 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104138 4805 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
127052466 140786 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 140786 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
44332701 4563 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL102490 4563 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
10276451 200285 37 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 200285 37 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 200285 37 None -2754 10 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
73213196 104460 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104460 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
44330514 208396 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99649 208396 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
119570 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3159 96 None -10 40 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
11026289 109534 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL322179 109534 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL5289845 194482 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 346 7 3 4 2.7 O=c1cc(CNC[C@@H](CO)Cc2ccsc2)[nH]c2ccc(F)cc12 10.1016/j.ejmech.2020.113141
155532148 171701 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4466677 171701 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL5082465 214804 0 None -239 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336062 5206 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106119 5206 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
35296170 142340 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL388620 142340 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
49799695 14398 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173436 14398 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200285 14398 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL5090346 215257 0 None -11 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
130431318 172383 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4476394 172383 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
168293190 192130 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 192130 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
11036641 31778 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL140612 31778 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10473658 187193 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 187193 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
44330567 208281 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98946 208281 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336036 4876 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104399 4876 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9841249 16395 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
CHEMBL123030 16395 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
9840412 118097 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
CHEMBL340669 118097 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
155538349 172376 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4476278 172376 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
145988180 165231 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 165231 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
164628817 186277 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 186277 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
56944383 112119 0 None -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 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 -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44405455 72368 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL198580 72368 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405489 132816 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370134 132816 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405466 166380 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL427555 166380 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
53364083 63854 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803053 63854 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
72545011 93126 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 93126 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137636460 156120 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 156120 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
137642380 158507 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 158507 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
11036641 31778 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 31778 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71734029 91055 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397392 91055 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
45272537 196526 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563614 196526 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
44393775 66304 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 66304 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
10200496 83593 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 83593 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
10473658 187193 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 187193 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
9909055 4842 4 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104238 4842 4 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
11325334 80051 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 80051 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
127031515 139434 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 139434 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
76314268 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
18414156 107086 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL315864 107086 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
18414156 107086 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL315864 107086 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
76314268 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 106434 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
11724450 123848 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123848 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123848 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
2728532 111554 3 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL328051 111554 3 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
76331467 85885 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298808 85885 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
10064981 205028 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL76982 205028 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44264629 97366 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL269576 97366 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44380685 58735 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168566 58735 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
25128757 103304 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 103304 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
134154387 152460 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 152460 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL5272829 193737 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 320 6 1 3 3.8 CCS[C@H]1CC[C@@H](N(C)CC(=O)Nc2ccc(C)c(C)c2)C1 10.1016/j.ejmech.2020.113141
164626655 186593 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 186593 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
145990141 166779 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283982 166779 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
60167309 75297 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 75297 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
60167309 75297 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
CHEMBL2037432 75297 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
11699469 77652 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
CHEMBL208847 77652 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
57402365 69295 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 69295 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
56837635 69308 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 69308 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57398875 69314 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 69314 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
127046950 140045 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 140045 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137643122 158035 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 158035 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
44459452 93893 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
CHEMBL24809 93893 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
19964406 114515 2 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 114515 2 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
10524751 57354 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL165171 57354 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
10543696 4581 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL102599 4581 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
51354277 60213 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688992 60213 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739996 60213 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
145993220 166764 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283709 166764 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
168277992 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5173368 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168277992 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
25139332 184319 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL484204 184319 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
127045853 139793 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139793 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
118709168 113415 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318840 113415 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189389 123244 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 123244 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
11694483 72243 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
CHEMBL198174 72243 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
90644069 112038 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289651 112038 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165537 75351 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037523 75351 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
10548967 112731 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
CHEMBL330470 112731 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
134154387 152460 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 152460 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
60167309 75297 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 75297 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
168277992 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5173368 190128 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
154724650 176337 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4543870 176337 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 176337 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
44192200 195389 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551964 195389 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
44396235 168537 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 168537 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
164622973 186123 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 186123 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
155564667 175481 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4577414 175481 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4444356 213932 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Nc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
9926401 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
16094676 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
5493357 206826 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL90466 206826 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
9952218 4881 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104432 4881 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
90644065 111661 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3286429 111661 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
12050194 202891 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL62703 202891 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
9926401 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 140875 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71061709 149527 0 None 3 11 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 149527 0 None 3 11 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
164611932 185202 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 185202 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
44427842 149808 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL394863 149808 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
168269421 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170670 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
49862238 15008 16 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
CHEMBL1209158 15008 16 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
5249956 73395 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 73395 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
44278111 100132 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL287671 100132 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
11957566 184 25 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
1219 184 25 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
3296 184 25 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
950 184 25 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
CHEMBL285755 184 25 None -79 9 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
168269421 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170670 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168269421 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 189962 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
53248212 62033 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 62033 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
44427831 92239 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL242644 92239 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
44438209 153962 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL398368 153962 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
9888555 165604 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 165604 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
10642239 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
44335907 5379 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107020 5379 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
44335800 110047 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL323525 110047 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
155537361 172298 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4475042 172298 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
155542182 173109 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4520460 173109 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71449737 81825 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164349 81825 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44405452 72556 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL199186 72556 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
53361301 63842 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803024 63842 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
21219154 88563 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL23537 88563 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
56926587 69010 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
CHEMBL1923416 69010 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
53361301 63842 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1803024 63842 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
10642239 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10642239 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 186659 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
9888555 165604 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
CHEMBL424294 165604 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
9861786 112345 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL329398 112345 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44273855 74402 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20251 74402 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
44273928 78081 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21011 78081 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10665101 101525 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 101525 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
10413085 83190 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218444 83190 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
127032383 139403 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 139403 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
10852461 206963 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91272 206963 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10449136 207431 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 207431 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10053476 116746 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
CHEMBL337531 116746 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
44380802 161691 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL413343 161691 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
127053220 139367 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 139367 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL5277325 193932 0 None 35 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 343 7 2 2 3.5 CN(C)[C@@H](CNC(=O)NC[C@H]1Cc2ccccc21)CC1CCCCC1 10.1016/j.ejmech.2020.113141
11849821 169300 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 169300 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
145991769 166881 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
CHEMBL4285984 166881 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
10476504 33487 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 33487 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
72545007 93122 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 93122 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
71456214 78686 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
CHEMBL2112466 78686 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
71457956 78424 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111527 78424 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
71454405 78425 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL2111528 78425 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44340415 8578 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8578 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
72205044 91945 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414355 91945 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
145979897 166606 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4280542 166606 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
15508243 5303 22 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL106635 5303 22 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10682854 24636 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL134326 24636 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44419056 83177 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
CHEMBL218368 83177 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
9930722 203672 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL67414 203672 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
9930722 203672 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL67414 203672 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
127050632 140743 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 140743 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
168282745 191095 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 191095 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
12581156 25150 17 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134759 25150 17 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
72164183 92151 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420778 92151 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
133633 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
177 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
CHEMBL445102 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
155195311 174347 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 174347 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
133633 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
177 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
CHEMBL445102 2241 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
44438235 93658 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL246854 93658 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
42626381 56245 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
CHEMBL1627315 56245 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
44431473 150739 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL395632 150739 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
44438197 153272 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 153272 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44304814 202872 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL62601 202872 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL5270705 193645 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 344 5 0 7 2.4 Cc1csc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)n1 10.1016/j.ejmech.2022.114840
44330564 107382 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL317825 107382 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336057 5908 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL107962 5908 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
168297637 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
9801858 63446 0 None -23 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL179757 63446 0 None -23 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
9817612 107256 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316942 107256 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
168297637 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5206427 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
44273876 79815 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
CHEMBL21205 79815 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
44517726 196022 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
CHEMBL560177 196022 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
168297637 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5206427 192323 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164622973 186123 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 186123 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
127051015 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11576528 84321 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221587 84321 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
9952528 99438 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
CHEMBL282927 99438 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
11191906 11767 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11767 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11767 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL5270705 193645 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 344 5 0 7 2.4 Cc1csc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)n1 10.1016/j.ejmech.2022.114840
127050632 140743 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 140743 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
126534204 138432 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 138432 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
154705884 176363 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4469584 176363 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 176363 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
71658072 90398 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386611 90398 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
44374431 54952 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161507 54952 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
10665626 112572 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL330100 112572 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
16104 161917 19 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL415300 161917 19 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
5311189 204841 11 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 204841 11 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
2389 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
2389 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 3331 118 None -22 67 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
9906071 16307 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
CHEMBL122597 16307 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
10854185 114539 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
CHEMBL333658 114539 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
155518026 170237 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4445706 170237 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
162653993 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3645619 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
975 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
CHEMBL45244 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
3251 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
127052487 140800 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140800 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
25070740 111775 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287391 111775 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
25072943 111777 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287393 111777 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
44431486 88073 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234645 88073 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
44405469 71986 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL197381 71986 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
72545240 93129 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 93129 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
44436602 145213 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL391256 145213 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
2 3261 23 None -2 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
54562 3261 23 None -2 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
CHEMBL240773 3261 23 None -2 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
122181329 121870 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 121870 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
71459759 84071 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207633 84071 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
45269168 195930 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL559399 195930 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
3251 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
127031519 139323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 139323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 139331 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 139331 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127052487 140800 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 140800 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
10612157 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL300571 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL423890 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
10612157 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL300571 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL423890 101857 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
162653993 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 183668 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3645619 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 3034 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
9982854 84340 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
CHEMBL221681 84340 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
10687967 205052 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77148 205052 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10039198 56349 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56349 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
15467372 169110 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL440120 169110 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
127032082 139317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 139317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127051015 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 140874 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
137635364 156260 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 156260 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4074669 156260 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
57391896 69305 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 69305 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57400557 69312 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 69312 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
118709170 113417 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318842 113417 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137645830 157852 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 157852 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
10924369 9336 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL111184 9336 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
11747350 107332 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 107332 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
2337 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
2337 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 3256 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL5075726 214395 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00611
44335635 4796 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104099 4796 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44381217 59146 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL169889 59146 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
44319368 106064 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 106064 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
11356479 71837 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 71837 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
10564794 57539 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL166325 57539 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
11615782 72226 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
CHEMBL198125 72226 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
154704368 176471 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4569006 176471 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 176471 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
135469096 12066 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183656 12066 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL309843 12066 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
71658074 90400 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386613 90400 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
76325764 106300 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3133866 106300 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3139064 106300 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
60167452 75354 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 75354 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167452 75354 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037526 75354 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
4064333 85740 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
4064333 85740 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL229019 85740 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229019 85740 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 708 37 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
7625 708 37 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
CHEMBL25236 708 37 None -109 19 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
60167452 75354 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 75354 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
127051016 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
49798839 14362 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172214 14362 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200154 14362 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
154703438 176381 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4475699 176381 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4595859 176381 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
127051016 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 140876 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
118719799 115726 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353902 115726 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
10893228 40214 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL148042 40214 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
145970938 165156 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 165156 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145992489 166977 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166977 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
9992499 73386 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 73386 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
168283295 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5189986 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
11566745 74694 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 74694 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 74694 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
168283295 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168275962 190619 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 190619 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
168291848 191872 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 191872 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
168283295 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5189986 191235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
168275089 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
71061729 160943 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4115493 160943 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
5025739 169196 45 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 169196 45 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
44438233 93610 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246643 93610 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168279825 190816 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 190816 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
44426511 137294 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL375238 137294 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
44330566 208280 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98945 208280 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
11133533 45217 0 None -17 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152587 45217 0 None -17 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
242 470 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
34 470 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
60795 470 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
CHEMBL1112 470 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
DB01238 470 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
11849736 138415 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 138415 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
44431471 168378 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL434583 168378 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
155195496 170716 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 170716 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
122442272 138348 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 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 -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 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 -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44330386 107374 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317770 107374 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL5270836 193656 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 377 5 1 5 3.9 Cc1csc(OC[C@@H]2CN(Cc3cc4ccc(Cl)cc4[nH]3)CCO2)n1 10.1016/j.ejmech.2022.114840
5311346 204154 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 204154 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 204154 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
168292124 192025 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 192025 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168290895 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5201507 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5270836 193656 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 377 5 1 5 3.9 Cc1csc(OC[C@@H]2CN(Cc3cc4ccc(Cl)cc4[nH]3)CCO2)n1 10.1016/j.ejmech.2022.114840
11453253 84314 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
CHEMBL221549 84314 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
22727351 12981 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1189537 12981 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL538977 12981 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122442272 138348 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 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 -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 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 -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL5288366 194420 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 433 5 1 3 4.6 Cc1c(Cl)cccc1NC(=O)CN1CCC2(CCCN2Cc2ccc(F)c(F)c2)C1 10.1016/j.ejmech.2022.114840
60167451 75348 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 75348 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
10456166 119633 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL346692 119633 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL4285942 119633 0 None -2754 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
44339984 167797 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167797 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10641955 206848 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
CHEMBL90569 206848 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
44394820 64851 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL182075 64851 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
44394629 65575 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL183160 65575 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
44214764 67199 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187804 67199 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
15522515 98161 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL273860 98161 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10641955 206848 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL90569 206848 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
44403232 71076 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL195247 71076 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
9949554 16853 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124835 16853 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
44395741 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL476935 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL558392 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
155567971 176021 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4589982 176021 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
9861462 83334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 83334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
52945819 17553 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258037 17553 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
137640391 156705 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 156705 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
21219167 99653 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL284346 99653 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
10665598 35083 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
CHEMBL143355 35083 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
22100964 203955 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL69356 203955 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44395741 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL476935 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL558392 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395741 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476935 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL558392 181581 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
44395741 181581 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL476935 181581 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL558392 181581 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
10015731 208169 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
CHEMBL98305 208169 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
127053217 139318 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 139318 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
11581443 96401 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL26188 96401 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
9837137 112326 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329276 112326 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
127031508 139381 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 139381 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
11624518 200343 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL597601 200343 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
145990453 166945 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287062 166945 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
168290895 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5201507 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168290895 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 191999 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
49783041 17171 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256171 17171 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
44436603 145216 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL391257 145216 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
44249745 195443 1 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL552373 195443 1 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL567286 195443 1 None -229 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
4420454 56259 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 56259 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44304603 203138 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64139 203138 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44304621 203419 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL65641 203419 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
10276451 200285 37 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 200285 37 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 200285 37 None -2754 10 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
131801154 170251 0 None -14 3 Human 6.8 pKi = 6.8 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 432 7 1 5 4.0 Cn1ccc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc21 10.1021/acs.jmedchem.1c00704
CHEMBL4445841 170251 0 None -14 3 Human 6.8 pKi = 6.8 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 432 7 1 5 4.0 Cn1ccc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc21 10.1021/acs.jmedchem.1c00704
44437897 153053 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397592 153053 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
11615489 69443 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 69443 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11708363 71902 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL197159 71902 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL5288366 194420 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 433 5 1 3 4.6 Cc1c(Cl)cccc1NC(=O)CN1CCC2(CCCN2Cc2ccc(F)c(F)c2)C1 10.1016/j.ejmech.2022.114840
60167451 75348 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 75348 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167451 75348 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037520 75348 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44338248 8351 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL109299 8351 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
155516494 170121 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 170121 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10438027 66188 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 66188 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
11408135 124188 0 None -39 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL363406 124188 0 None -39 3 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
168275089 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5179198 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
168292951 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5203807 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168292951 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168292951 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5203807 192148 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
44582676 189779 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189779 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44393658 124095 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL363308 124095 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
168275089 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5179198 190496 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
118643968 145970 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL3918282 145970 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
118643968 145970 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3918282 145970 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
42626317 56252 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627322 56252 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
44350664 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL340816 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553417 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44350664 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL340816 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553417 118149 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9931571 5335 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106827 5335 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL5086564 215035 0 None -316 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
71658204 90405 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386618 90405 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
11351639 60524 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
CHEMBL175734 60524 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
11351639 60524 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 60524 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
56593482 3941 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3941 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3941 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
3037308 44079 27 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 44079 27 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
154727843 176433 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4448853 176433 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 176433 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
44394590 127549 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366304 127549 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
71458071 79500 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 79500 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
10735405 207411 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93958 207411 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10947658 28702 0 None -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
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 -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
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
44278789 99917 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL286177 99917 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
4088306 100638 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29206 100638 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
135481864 12350 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 12350 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 12350 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
10837494 207454 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL94200 207454 0 None 8 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155516873 170128 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4443944 170128 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
25072635 111783 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111783 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
11720302 166258 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL426863 166258 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
21219156 95826 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL25887 95826 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
44376241 120115 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351098 120115 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
135398737 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
38 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
722 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
CHEMBL42 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
DB00363 958 93 None -13 89 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
127032083 139447 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 139447 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
9967004 39357 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147130 39357 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
44591045 176737 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
CHEMBL460223 176737 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
11681599 75173 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 75173 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
44380697 58093 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167414 58093 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
11624518 200343 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL597601 200343 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
60165413 75360 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037531 75360 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
122189392 123247 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 123247 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
122177642 121210 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 121210 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11348526 6361 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
CHEMBL108211 6361 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
10786474 207170 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92411 207170 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44371996 53623 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL160266 53623 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
11223708 166309 0 None -11 3 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL427173 166309 0 None -11 3 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
44263882 97225 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268558 97225 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
45482180 197904 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL572867 197904 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
25139478 184956 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL485384 184956 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44319361 205720 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 205720 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL5084145 214898 0 None -977 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
21559988 113427 3 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318852 113427 3 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
168279082 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5182602 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
168279082 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
44431485 88072 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234644 88072 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44415569 165934 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 165934 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
168279082 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5182602 190733 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
51354275 60184 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689012 60184 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739787 60184 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
12280580 44069 2 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL15146 44069 2 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
71062889 148274 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL3936595 148274 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
10894276 41323 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148965 41323 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
168280464 190736 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 190736 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
154703764 176310 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4455719 176310 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595265 176310 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
71458739 81823 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164347 81823 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
16090821 81833 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 81833 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
53248673 66404 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813591 66404 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851831 66404 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
90644071 112042 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 112042 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
37461 17134 14 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
CHEMBL1255588 17134 14 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
10436285 101952 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL301242 101952 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
1599 2341 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
3955 2341 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
7215 2341 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL841 2341 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
DB00836 2341 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10436285 101952 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 101952 0 None -954 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
118719796 115723 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353899 115723 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
164608999 184384 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 184384 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
71659909 90391 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386604 90391 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
168271806 190519 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 190519 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
44415690 80137 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 80137 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
164608999 184384 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 184384 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
135887931 12067 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183657 12067 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL309858 12067 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
122205437 137311 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 137311 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
71658073 90399 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386612 90399 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
72191067 92356 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430439 92356 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
10497179 205111 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL77743 205111 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
135492584 11333 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 11333 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 11333 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
44380715 59013 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169222 59013 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
10639353 114796 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL333983 114796 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155560295 175047 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4567758 175047 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
10224165 169059 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL439646 169059 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
135398745 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
52947756 17170 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256170 17170 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11742798 97113 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26758 97113 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
53364154 63843 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803025 63843 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53364227 63847 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803029 63847 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363202 63856 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803055 63856 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
118709176 113424 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318849 113424 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137644833 158139 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 158139 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
71459760 84072 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207634 84072 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
13091273 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL478617 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553327 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
127053219 139464 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 139464 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
13091273 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL478617 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553327 182438 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL5083441 214859 0 None 9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(O)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
90644062 112034 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 112034 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44372296 119487 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
CHEMBL345357 119487 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
10690882 197534 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL57019 197534 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
10548329 202628 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61248 202628 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273741 78507 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21119 78507 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
137644962 158493 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 158493 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
135398745 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2914 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
11779642 206859 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90654 206859 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
25139479 184317 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 184317 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
57390119 69303 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 69303 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
137655556 158539 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4091507 158539 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
44436610 91949 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241436 91949 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
52937777 61171 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL1765630 61171 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL5289063 194455 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccc5ccnn5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.1c00704
155562543 175172 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 175172 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
10667966 57160 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL164736 57160 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
42626240 56237 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627307 56237 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
11626748 140159 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
CHEMBL380287 140159 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
155562543 175172 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 175172 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
22910005 11599 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180629 11599 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL135395 11599 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
25141535 56238 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627308 56238 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
10515841 208265 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
CHEMBL98836 208265 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
71062567 160415 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111349 160415 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168280776 191158 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 191158 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
134136246 142538 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 142538 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
134136246 142538 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 142538 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
44438227 93555 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246437 93555 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25130157 103307 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 103307 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
130431303 172937 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4516799 172937 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
3246443 37686 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 37686 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
1353 1911 93 None -3 83 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1911 93 None -3 83 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1911 93 None -3 83 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1911 93 None -3 83 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1911 93 None -3 83 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
22727335 13485 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193307 13485 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544689 13485 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
168280974 190863 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 190863 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
10524285 202421 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61090 202421 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42273483 165295 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL423287 165295 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
75306277 109254 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109254 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
168275381 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5175548 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
11384664 83112 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
CHEMBL218203 83112 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
153287574 175247 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 175247 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10245409 49789 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL156732 49789 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
44214767 67042 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187122 67042 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394666 125792 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL364782 125792 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394742 166121 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL426062 166121 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
210956 206744 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL89970 206744 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10570080 107134 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
CHEMBL316125 107134 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
210956 206744 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL89970 206744 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
9840365 108452 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL31991 108452 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 205302 23 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7927 205302 23 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44336061 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL320597 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/j.ejmech.2020.113141
792265 92154 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420781 92154 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
9860183 107229 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316727 107229 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10588194 18920 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128524 18920 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
44336061 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL320597 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44335889 107354 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
CHEMBL317670 107354 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
44336074 4894 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104497 4894 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
44335812 4938 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104716 4938 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44336074 4894 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL104497 4894 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.ejmech.2020.113141
11464857 4781 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1016/j.ejmech.2020.113141
CHEMBL104035 4781 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1016/j.ejmech.2020.113141
137659990 159230 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 159230 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
122180955 121770 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589576 121770 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11559581 78418 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL211135 78418 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10476504 33487 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 33487 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
11464857 4781 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
CHEMBL104035 4781 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
44376209 56332 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL163009 56332 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44336061 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL320597 108621 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
119570 3159 96 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3159 96 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3159 96 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3159 96 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3159 96 None -10 40 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
10571927 207414 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
CHEMBL93970 207414 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
9802631 111997 1 None 10 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL328866 111997 1 None 10 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10716980 207837 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
CHEMBL96369 207837 0 None 2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
18624462 166943 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
CHEMBL428705 166943 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
10831735 31755 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140594 31755 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
137655636 158736 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 158736 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
10784211 104182 0 None 223 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL309730 104182 0 None 223 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
778880 50347 11 None 26 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
CHEMBL157222 50347 11 None 26 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
127032384 139376 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 139376 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
137643309 158415 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 158415 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10336538 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 1625 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
1353 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
3559 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
86 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
CHEMBL54 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
DB00502 1911 93 None -3 83 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
45361874 170021 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
168285560 192918 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 192918 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 192918 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
3303 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 2244 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
10404144 205302 23 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
CHEMBL7927 205302 23 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
1353 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
3559 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
86 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
CHEMBL54 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
DB00502 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
9847013 45360 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL15270 45360 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
1353 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
3559 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
86 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
CHEMBL54 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
DB00502 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
11811808 45417 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152756 45417 0 None -5 4 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
3645619 3034 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
975 3034 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
CHEMBL45244 3034 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
27620 140818 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 140818 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
46893146 61607 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 61607 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
137634397 156105 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 156105 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
1353 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
3559 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
86 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
CHEMBL54 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
DB00502 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
11633170 78412 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
CHEMBL211118 78412 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
45273045 196376 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 196376 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10361512 54439 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 54439 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
10267394 100389 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28997 100389 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
1353 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
3559 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
86 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
CHEMBL54 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
DB00502 1911 93 None -3 83 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
10042972 106540 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
CHEMBL314095 106540 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
10042972 106540 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1016/j.ejmech.2020.113034
CHEMBL314095 106540 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1016/j.ejmech.2020.113034
21533446 70155 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 70155 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
21527771 70156 1 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940404 70156 1 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
71463207 84074 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207636 84074 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135524323 195426 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
CHEMBL552268 195426 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
9863333 204365 0 None -1 10 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71724 204365 0 None -1 10 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
44340333 9662 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9662 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
5029739 100826 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL293341 100826 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
13869641 113403 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318824 113403 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9949442 95584 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL25772 95584 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
5029739 100826 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
CHEMBL293341 100826 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
71583848 87731 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87731 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
133008 2242 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
3302 2242 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL444309 2242 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
44412468 165930 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL425057 165930 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
10640530 112289 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
CHEMBL329126 112289 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
44323962 206830 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
CHEMBL90476 206830 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
10807795 39270 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL147059 39270 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
10664621 43962 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL151286 43962 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
76320592 85886 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
CHEMBL2298809 85886 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
10404144 205302 23 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
CHEMBL7927 205302 23 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
10640530 112289 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL329126 112289 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1016/j.ejmech.2020.113034
155510756 169512 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4434714 169512 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
155564308 175153 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4570073 175153 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
44412468 165930 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL425057 165930 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44371932 119648 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL346805 119648 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
168268770 192772 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5169993 192772 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221238 192772 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788870 18258 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270322 18258 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10589218 21210 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131299 21210 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44270558 165288 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL423247 165288 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
44339992 109184 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 109184 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10336538 1625 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 1625 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 1625 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
10646459 207132 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
CHEMBL92199 207132 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
10589218 21210 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL131299 21210 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
11724450 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
44412269 78100 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL210232 78100 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44412269 78100 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210232 78100 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
11724450 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 123848 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44270558 165288 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL423247 165288 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
119570 3159 96 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3159 96 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3159 96 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3159 96 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3159 96 None -10 40 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
6469693 79955 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL212631 79955 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
10854370 119606 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL346398 119606 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
18403576 6191 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1016/j.ejmech.2020.113141
CHEMBL108122 6191 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1016/j.ejmech.2020.113141
54583897 61602 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771106 61602 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
6469693 79955 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79955 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
44241718 195264 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL551199 195264 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10249308 4903 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104550 4903 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
15512070 53242 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL159903 53242 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372338 53846 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160454 53846 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44278115 101519 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL29808 101519 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
137649896 157533 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4080034 157533 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
137649896 157533 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
CHEMBL4080034 157533 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
14925759 158038 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL4085780 158038 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
14925759 158038 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158038 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44412494 78321 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210955 78321 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
17475863 168784 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL437490 168784 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
44323763 206493 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL88289 206493 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
76309673 85889 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298812 85889 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
60785 205893 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
CHEMBL83894 205893 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
155534246 171931 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4470231 171931 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
155566058 175700 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4582096 175700 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
54581964 61608 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771111 61608 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
60785 205893 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
CHEMBL83894 205893 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
44412494 78321 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210955 78321 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
17475863 168784 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL437490 168784 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
11372852 5128 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105696 5128 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
49788942 18289 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270516 18289 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
10691523 105610 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL312255 105610 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
10837493 207104 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL92030 207104 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155547128 173661 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4534703 173661 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
90644062 112034 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 112034 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49782600 17453 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257689 17453 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
10548329 202628 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL61248 202628 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
72544566 93131 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 93131 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
25333445 78123 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210318 78123 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
122191605 123720 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 123720 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
44376230 119987 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349904 119987 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372296 119487 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL345357 119487 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
71450812 78422 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111525 78422 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11849776 79772 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 79772 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
667675 205132 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77969 205132 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
9820085 141330 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38349 141330 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
44340186 9660 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9660 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
44380770 165712 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL424575 165712 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
3156990 8130 22 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL109173 8130 22 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
76441180 115737 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353913 115737 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
11658914 70240 1 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 70240 1 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
11405182 108534 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL320071 108534 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
56597938 3940 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3940 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3940 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
168275381 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
44415672 80174 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 80174 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
42605994 17874 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 17874 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
9865384 173495 35 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL45305 173495 35 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
56658008 66420 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813599 66420 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851895 66420 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
10572229 121017 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
CHEMBL356542 121017 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
168275381 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5175548 190270 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
154725766 176645 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4527244 176645 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4598000 176645 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL5094044 215464 2 None -30 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10737150 107536 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL318747 107536 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168294958 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5207898 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
127051844 140847 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140847 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
42626172 56244 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
CHEMBL1627314 56244 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
162659314 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
127051844 140847 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 140847 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
168294958 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
11771801 80029 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 80029 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
162659314 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 183696 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
22953120 108469 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL319927 108469 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
168294958 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5207898 192404 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
1212 1662 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
168285068 191583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 191583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
154705038 176646 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4584481 176646 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 176646 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
168285068 191583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5195130 191583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
168289523 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5193761 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
127051845 140729 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140729 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10551026 101617 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101617 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44301054 196148 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 196148 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
135398737 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
38 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
722 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
CHEMBL42 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
DB00363 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
135398737 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
38 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
722 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
CHEMBL42 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
DB00363 958 93 None -13 89 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
135418440 12068 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 12068 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 12068 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
3802 203023 21 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
CHEMBL63329 203023 21 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
21830793 91835 10 None -138 45 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91835 10 None -138 45 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
9930934 108637 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
CHEMBL320721 108637 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
44336109 110950 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326202 110950 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
2435 3590 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 3590 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 3590 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 3590 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 3590 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
9905246 16338 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
CHEMBL122862 16338 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
155563950 175273 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4572646 175273 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127028181 139449 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 139449 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
57391216 70168 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 70168 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391216 70168 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940416 70168 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
44431490 88272 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234826 88272 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
44405490 133450 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL370652 133450 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
137659303 159304 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 159304 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
22100932 204095 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL70215 204095 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
45273442 196451 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL563078 196451 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44276075 13225 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191252 13225 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542325 13225 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
10715225 207118 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92121 207118 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44400594 133575 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL371165 133575 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
11948707 166167 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
CHEMBL426317 166167 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
10616050 186646 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 186646 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
57326583 74063 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022271 74063 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
127051845 140729 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 140729 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44426512 85745 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229076 85745 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
14665503 91234 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL240106 91234 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
9977478 204943 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL76402 204943 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
137632607 156339 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4065797 156339 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
1577 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
2537 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5355 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5501 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
643497 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
688272 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
958 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
960 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL196677 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL26 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL267044 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB00391 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB16021 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
51354851 60174 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688994 60174 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739761 60174 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
44578445 181579 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476933 181579 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
1577 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
2537 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5355 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5501 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
643497 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
688272 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
958 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
960 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL196677 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL26 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL267044 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB00391 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB16021 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
137633454 156591 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4068702 156591 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
1577 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
2537 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5355 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5501 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
643497 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
688272 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
958 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
960 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL196677 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL26 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL267044 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB00391 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB16021 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
168289523 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5193761 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
168289523 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 191499 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
10692886 53654 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL160296 53654 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813590 53654 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
4797946 170424 7 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 170424 7 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168275717 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5174731 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
2247 505 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
763774 92149 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420776 92149 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
42626313 56247 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627317 56247 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
10161526 13303 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191882 13303 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL543040 13303 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
44438232 148781 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394066 148781 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
154705296 176394 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4444691 176394 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 176394 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
168275717 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5174731 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
168275717 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 190219 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
11133385 102186 0 None -25 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL302796 102186 0 None -25 5 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154706703 176232 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4550187 176232 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4594691 176232 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
154706461 176348 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4470439 176348 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 176348 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
10613605 200948 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
CHEMBL60185 200948 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
10617381 189686 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 189686 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11649431 165982 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL425285 165982 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
10688035 104769 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310819 104769 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
4420454 56259 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 56259 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10616050 186646 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 186646 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10131111 208326 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99208 208326 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
10041417 26418 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135954 26418 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10740968 96723 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26426 96723 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44405451 135348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL372770 135348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
9908125 119344 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
CHEMBL344270 119344 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
44436597 91800 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241210 91800 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
71734127 91057 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397476 91057 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
46917637 68332 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 68332 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
10861560 45333 10 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
CHEMBL152679 45333 10 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
11280344 92157 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420891 92157 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44283941 137930 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
CHEMBL37638 137930 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
11324794 138259 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 138259 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
90644063 112035 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 112035 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 112035 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 112035 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
76328715 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
133633 2241 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
177 2241 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
CHEMBL445102 2241 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
44380774 120475 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL354180 120475 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
154704141 176679 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4561808 176679 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598299 176679 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49783042 17691 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258495 17691 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57390115 69296 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 69296 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
44436601 91943 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL241424 91943 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
10830804 207922 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
CHEMBL96792 207922 0 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
2337 3256 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3256 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3256 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3256 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3256 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
10438027 66188 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
CHEMBL184383 66188 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
142590710 180270 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4750607 180270 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
118709166 113412 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318838 113412 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12071089 5305 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
CHEMBL106660 5305 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
122180610 121738 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588981 121738 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44426513 85746 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229077 85746 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
154706546 176446 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4452329 176446 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596339 176446 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
44431472 87482 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233403 87482 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
49799713 14409 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173778 14409 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200306 14409 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
162666450 182289 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 182289 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
10225942 13154 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190732 13154 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL541524 13154 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
45379370 7523 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 7523 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
16744003 92558 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243225 92558 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
162666450 182289 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 182289 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
17755866 142884 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 142884 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
9929581 16514 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL123663 16514 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
118719810 115738 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353914 115738 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44438222 93491 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246230 93491 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10425024 7136 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
CHEMBL108531 7136 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
9794644 107281 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317078 107281 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
127051863 140814 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818940 140814 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
10425024 7136 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL108531 7136 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL5283077 194185 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 0 5 2.9 c1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)nc1 10.1016/j.ejmech.2022.114840
CHEMBL5283077 194185 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 0 5 2.9 c1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)nc1 10.1016/j.ejmech.2022.114840
44438219 167673 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL430198 167673 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10688036 104145 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL309460 104145 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10735344 104858 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310985 104858 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10381810 205174 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7828 205174 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
44381118 57569 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL166587 57569 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
44356064 116546 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL336295 116546 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
90644063 112035 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 112035 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 112035 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 112035 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49783040 17690 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
CHEMBL1258494 17690 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
72544789 93132 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 93132 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
11417962 4974 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104873 4974 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10832341 207853 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96462 207853 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168278360 192847 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5188796 192847 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221749 192847 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
11089541 84386 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2112905 84386 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2219567 84386 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
9883554 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10071413 83970 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL220700 83970 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
35295787 85741 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229021 85741 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44336571 4831 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL104201 4831 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
52937680 61173 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
CHEMBL1765632 61173 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
9838216 203188 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL64283 203188 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
130431279 175884 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4586327 175884 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
44264741 204742 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7441 204742 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
10300403 13730 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1195074 13730 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL553810 13730 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122180575 121727 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588920 121727 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
24060 119655 12 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL346898 119655 12 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154725813 176526 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4568916 176526 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 176526 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
44276079 13800 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1195587 13800 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL554897 13800 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
56664952 66384 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813598 66384 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851753 66384 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
9928332 97180 5 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL268258 97180 5 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL5083186 214850 0 None -1202 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336172 5361 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106917 5361 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336194 107539 1 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL318760 107539 1 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
122181334 121876 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
CHEMBL3590086 121876 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
130431317 172950 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 172950 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
164628177 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
168281091 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5187429 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
10404657 98069 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 98069 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
11213037 137103 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
CHEMBL374749 137103 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
71618702 143382 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
CHEMBL3897835 143382 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
90644070 112041 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289654 112041 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
164628177 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 188611 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44394636 66918 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL186558 66918 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
44214765 165800 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL424808 165800 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
219050 3373 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
52 3373 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
CHEMBL431367 3373 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
13015797 205897 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
CHEMBL83915 205897 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
9888555 165604 16 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
CHEMBL424294 165604 16 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
136056636 111788 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111788 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709159 113405 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318831 113405 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11156017 5126 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105686 5126 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
9927411 203053 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL63576 203053 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
9797200 118971 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL34239 118971 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
45482153 198038 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL574030 198038 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
44380785 120803 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL355566 120803 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
10404657 98069 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 98069 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
90644064 112036 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289649 112036 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
57390117 69299 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 69299 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
127047221 139930 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139930 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
57400562 69318 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 69318 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
71086389 160408 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111289 160408 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
10811814 207465 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL94265 207465 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
154704941 176627 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4578364 176627 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597877 176627 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
168281091 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5187429 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
10811814 207465 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL94265 207465 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168281091 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 191071 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
182600 118744 2 None -2 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
CHEMBL341774 118744 2 None -2 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
10229397 13256 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1191467 13256 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL542571 13256 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
44438215 93410 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
CHEMBL245816 93410 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
9906978 42711 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42711 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
49798812 14320 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170456 14320 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199971 14320 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
9906978 42711 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42711 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
23290944 81826 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81826 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
51353989 60209 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689006 60209 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739963 60209 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
9908071 203004 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL63209 203004 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
21533446 70155 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940403 70155 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
90181059 160231 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL4109801 160231 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
44339879 172282 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 172282 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
11792324 205729 0 None 8 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL82591 205729 0 None 8 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10851078 199390 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59103 199390 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
10644771 107089 0 None -61 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL315879 107089 0 None -61 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
44335761 109221 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321734 109221 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10851078 199390 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59103 199390 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
145988693 167166 0 None 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
45268293 196135 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL561123 196135 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10644771 107089 0 None -61 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL315879 107089 0 None -61 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44301157 101706 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
CHEMBL299479 101706 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
10595646 199357 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59075 199357 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42266974 99295 9 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL282008 99295 9 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 919 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 919 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 919 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 919 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 919 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
11185987 80348 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 80348 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094666 81727 3 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 81727 3 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL5089655 215220 0 None 2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10089203 41353 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14899 41353 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
233199 155611 16 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL404570 155611 16 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44380717 120349 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353087 120349 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
23642427 91799 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL241169 91799 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
57395340 69300 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 69300 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
11774358 5153 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105836 5153 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12049520 101065 5 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL294780 101065 5 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
10449136 207431 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 207431 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10014924 107271 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 107271 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 107271 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 107271 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
18519 67660 27 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
CHEMBL19068 67660 27 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
134155116 150968 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 150968 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
242 470 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 470 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 470 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 470 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 470 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
155547197 173595 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 173595 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134155116 150968 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 150968 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
11540842 84373 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL221897 84373 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
9872676 78195 0 None -6309 16 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 78195 0 None -6309 16 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
11522476 74523 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 74523 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
71453386 81821 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164345 81821 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
4987774 14359 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172210 14359 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200151 14359 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
10801925 11624 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180675 11624 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL138016 11624 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
44330340 107475 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL318415 107475 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
46227317 200163 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 200163 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
155547197 173595 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 173595 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
11633816 13125 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190494 13125 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541025 13125 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
137640511 157066 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 157066 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
23363843 109671 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL322567 109671 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
44370058 119694 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347291 119694 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10357628 13923 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1196433 13923 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL556969 13923 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10474613 163291 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL418758 163291 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10176799 208262 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98830 208262 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
127029389 139443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 139443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
44431488 88075 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL234647 88075 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
22100933 204290 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71324 204290 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44371980 53935 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160536 53935 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
1353 1911 93 None -3 83 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
3559 1911 93 None -3 83 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
86 1911 93 None -3 83 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL54 1911 93 None -3 83 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
DB00502 1911 93 None -3 83 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
11220975 102993 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL306711 102993 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
5311346 204154 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL1256778 204154 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL70565 204154 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
10665101 101525 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 101525 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
9883554 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10498972 118459 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL341225 118459 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
44269825 42512 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14998 42512 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL5277859 193955 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 348 4 0 5 2.8 CCOC(=O)N1CCN(Cc2cnn(-c3ccc(Cl)cc3)c2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL5277859 193955 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 348 4 0 5 2.8 CCOC(=O)N1CCN(Cc2cnn(-c3ccc(Cl)cc3)c2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL4434865 213923 1 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None c1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
25141534 56235 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
CHEMBL1627305 56235 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
25141534 56235 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627305 56235 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
137637428 156236 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4064759 156236 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5076359 214432 0 None -77 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None COc1cccc(C(=CCNCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2cccc(OC)c2)c1 10.1021/acs.jmedchem.1c00611
181743 178572 5 None -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 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 -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
1605 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
1728 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
22267 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
4095 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
4586 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
5458 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL159659 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL651 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
DB00333 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
DB13515 2498 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
11488451 203150 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
CHEMBL64176 203150 0 None -12 3 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
10782097 114264 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
CHEMBL333057 114264 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
511484 4344 71 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL101032 4344 71 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
142590755 183426 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
CHEMBL4798638 183426 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
CHEMBL5274285 193806 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 415 4 1 2 5.3 Fc1ccc(CN2CCCC23CCN(Cc2cc4ccc(Cl)cc4[nH]2)C3)cc1F 10.1016/j.ejmech.2022.114840
10058787 116594 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL336652 116594 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
122180611 121739 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588982 121739 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
134154680 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL5274285 193806 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 415 4 1 2 5.3 Fc1ccc(CN2CCCC23CCN(Cc2cc4ccc(Cl)cc4[nH]2)C3)cc1F 10.1016/j.ejmech.2022.114840
11613105 84068 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL220754 84068 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
44339992 109184 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 109184 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10665101 101525 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 101525 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
9883554 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 165354 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10498972 118459 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL341225 118459 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
44336313 9244 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL110712 9244 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
9883552 15586 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL122140 15586 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
127031497 139491 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 139491 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
145969667 164965 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164965 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
118709751 113541 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113541 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
21219144 93340 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24539 93340 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10939167 9500 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 9500 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL129483 9500 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
44332566 108359 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL319816 108359 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
56681927 66396 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813593 66396 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851787 66396 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
11221906 79911 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 79911 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
76328715 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 106372 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
9841608 100423 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL290351 100423 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
10449136 207431 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL94067 207431 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10449136 207431 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 207431 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
137640836 157006 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
CHEMBL4073330 157006 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
17987129 111419 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327339 111419 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014681 204729 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7430 204729 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
44323876 206582 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL88870 206582 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10568740 15556 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121967 15556 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
15508239 6256 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL108160 6256 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
44582678 181574 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 181574 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
17756101 98584 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 98584 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
134154680 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 154562 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
9904074 110628 3 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
CHEMBL325710 110628 3 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
44330692 112368 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329503 112368 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10357631 7989 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
CHEMBL109063 7989 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
168296363 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5209344 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
155557792 174685 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
CHEMBL4559278 174685 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
44438218 93449 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246020 93449 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168296363 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5209344 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168296363 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 192517 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
17756212 86368 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 86368 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
7077 66959 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 66959 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL3925724 66959 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
15034333 4250 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL100461 4250 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
44591042 176811 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL460854 176811 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
10357631 7989 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL109063 7989 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL5087543 215107 0 None -46 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
134153539 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
10017758 13184 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1190993 13184 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL542029 13184 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
45482169 197838 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
CHEMBL572379 197838 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
135398745 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
135398745 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
155548336 173740 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4536530 173740 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127029391 139348 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 139348 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL5282085 194142 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 5 3.1 Cn1ncc2cc(CN3CCO[C@H](COc4ccc(F)c(F)c4)C3)ccc21 10.1016/j.ejmech.2022.114840
118709750 113540 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 113540 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
16105548 82698 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL217964 82698 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL221652 82698 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
10073194 12963 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189407 12963 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL538723 12963 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
135398745 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
47 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
CHEMBL715 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
DB00334 2914 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
118714552 114527 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 114527 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
10430935 105794 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3126735 105794 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL5282085 194142 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 5 3.1 Cn1ncc2cc(CN3CCO[C@H](COc4ccc(F)c(F)c4)C3)ccc21 10.1016/j.ejmech.2022.114840
155536720 172187 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 172187 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 958 93 None -13 89 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 958 93 None -13 89 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 958 93 None -13 89 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 958 93 None -13 89 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 958 93 None -13 89 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
57399432 70465 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946254 70465 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57399432 70465 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946254 70465 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
137635734 156112 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 156112 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44336552 111340 1 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL326864 111340 1 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10573099 207828 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96322 207828 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
164628883 186451 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4876546 186451 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
11652518 165932 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL425064 165932 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
16277250 110492 4 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL324867 110492 4 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44426510 85744 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229025 85744 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
134153539 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 154505 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
11384207 83352 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
CHEMBL219274 83352 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
11569619 136563 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL373873 136563 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
11670421 168795 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL437525 168795 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
90644072 112039 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289652 112039 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
44438186 147208 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL392822 147208 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
11016342 102804 0 None -281 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
CHEMBL305362 102804 0 None -281 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
76311262 106293 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133779 106293 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139053 106293 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
71061724 145552 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 145552 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
56664950 66625 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1813592 66625 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1852737 66625 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
155195311 174347 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 174347 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
44330554 208222 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98578 208222 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
17756102 86144 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 86144 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
11512263 84367 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL221866 84367 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
154726529 176445 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4467486 176445 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596338 176445 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
10469437 56541 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL163863 56541 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
135398737 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
30740059 107668 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
CHEMBL319043 107668 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
135398745 2914 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 2914 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 2914 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 2914 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
44335813 5359 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106914 5359 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
127030612 139330 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 139330 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
10115074 120674 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL354699 120674 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
25070416 111785 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
CHEMBL3287401 111785 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
44426508 85742 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229023 85742 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
118709174 113422 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318847 113422 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10641637 118780 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL342001 118780 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
11290928 5306 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106665 5306 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44372198 49140 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL156198 49140 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
162671033 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44264622 97143 4 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL267853 97143 4 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
122177644 121212 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 121212 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
44335569 5159 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
CHEMBL105894 5159 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
44319370 107047 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 107047 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
13014680 98445 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL275696 98445 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1499 2091 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 2091 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 2091 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 2091 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 2091 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
71462266 81831 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164355 81831 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
154706513 176586 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4440698 176586 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 176586 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
10803829 11605 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180636 11605 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135725 11605 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
57587922 171512 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL4464060 171512 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL5077114 214482 0 None -2137 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
155195486 169687 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 169687 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
16094677 83336 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 83336 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
9929629 102116 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL302340 102116 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44332581 4381 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
CHEMBL101285 4381 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
71658075 90401 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386614 90401 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
109030343 170860 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170860 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
122180568 121720 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588913 121720 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
163322331 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5204764 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
44431492 88276 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234827 88276 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
11637457 73087 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 73087 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
163322331 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44438230 93557 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 93557 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
10021193 66363 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 66363 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
44214766 67065 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187236 67065 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
11559589 122707 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL360424 122707 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
72901200 119777 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210307
CHEMBL3480577 119777 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210307
9995379 106950 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL314952 106950 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
135887940 11335 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL1179506 11335 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL80711 11335 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
44264642 204803 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7506 204803 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
10454684 204805 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7508 204805 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
9909648 205573 3 None -1 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81330 205573 3 None -1 12 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
9995379 106950 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL314952 106950 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
10836365 207263 0 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL93021 207263 0 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
231915 92158 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420892 92158 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
10220333 4207 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL100203 4207 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
44336030 5211 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL106169 5211 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
10001810 5341 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106862 5341 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335919 108928 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321121 108928 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
1946142 109621 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL322222 109621 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
44335739 4847 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
CHEMBL104273 4847 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
9799123 5619 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 5619 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44336006 6251 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108157 6251 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
72901200 119777 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
CHEMBL3480577 119777 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
9909648 205573 3 None 1 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constant
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL81330 205573 3 None 1 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constant
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
54581963 61601 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771105 61601 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
11559589 122707 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL360424 122707 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
135921193 40194 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
CHEMBL148024 40194 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
9909648 205573 3 None 1 12 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL81330 205573 3 None 1 12 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
10684706 85722 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL22892 85722 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10617366 205442 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80318 205442 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
10404144 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
10980338 168008 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
CHEMBL432059 168008 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
10336538 1625 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
974 1625 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
CHEMBL310843 1625 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
10684706 85722 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL22892 85722 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11003833 44763 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152159 44763 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
10404144 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL7927 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.ejmech.2020.113141
10404144 205302 23 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL7927 205302 23 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
21219164 91550 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24051 91550 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
12052258 100094 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL287412 100094 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10404144 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 205302 23 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
9840672 206317 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87192 206317 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
2780 110529 36 None -4 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
CHEMBL325109 110529 36 None -4 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
44412458 139294 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL379177 139294 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
9821010 55455 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161982 55455 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44419066 84362 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
CHEMBL221814 84362 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
44340227 110641 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110641 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10574818 207901 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
CHEMBL96703 207901 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
1353 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -3 83 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -3 83 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -3 83 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -3 83 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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
9948461 19501 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL129931 19501 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155532505 171758 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4467437 171758 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
127028185 139336 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 139336 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
127032383 139403 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL3793438 139403 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
54580906 61605 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 61605 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363109 63848 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803030 63848 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
1353 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
3559 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
86 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
CHEMBL54 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
DB00502 1911 93 None -3 83 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
22065997 99355 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL282424 99355 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
44400500 166060 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL425731 166060 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
127032383 139403 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL3793438 139403 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
10593191 189108 1 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 189108 1 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
44394667 67039 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL187113 67039 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
10741841 207080 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
CHEMBL91859 207080 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
977 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
9820261 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
CHEMBL66227 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
155513773 169824 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4439644 169824 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
54580905 61603 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 61603 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53327908 61609 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771112 61609 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10594054 31413 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL140258 31413 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
45268292 196687 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL564688 196687 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
977 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
9820261 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
CHEMBL66227 1178 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
10473658 187193 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 187193 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
1524 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
197 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
3822 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
88 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
CHEMBL51 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
DB12465 2181 96 None -4 52 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
44209480 70170 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL1940418 70170 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
134135650 144366 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
CHEMBL3905761 144366 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
44209480 70170 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL1940418 70170 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44209480 70170 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 70170 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209480 70170 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940418 70170 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
15817410 57535 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166269 57535 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
134135650 144366 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
CHEMBL3905761 144366 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
168275783 192827 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5176100 192827 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221583 192827 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
9995264 207183 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL92489 207183 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
10691599 202589 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
CHEMBL61195 202589 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
44278788 110338 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL32402 110338 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
CHEMBL7927 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
10404144 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
CHEMBL7927 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
CHEMBL146246 38278 0 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
9995264 207183 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL92489 207183 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
9906978 42711 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 42711 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9906978 42711 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 42711 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
973 1177 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 1177 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 1177 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
188942 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
3297 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
979 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
CHEMBL103772 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
155515931 170011 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442470 170011 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
1353 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
3559 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
86 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
CHEMBL54 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
DB00502 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
10691599 202589 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
CHEMBL61195 202589 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
10567430 119293 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL343880 119293 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
10404144 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
CHEMBL7927 205302 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
9905249 99902 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28607 99902 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
133079 3638 42 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
980 3638 42 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL69759 3638 42 None 1 4 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
44454734 97727 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL271513 97727 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
3303 2244 46 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
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 -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
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 -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
10545941 38925 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL146757 38925 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
188942 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
3297 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
979 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
CHEMBL103772 2818 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
44326212 207428 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
CHEMBL94050 207428 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
155512259 169648 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4437233 169648 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
132060812 162036 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 162036 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
71450707 84078 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 84078 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
45273443 195631 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL556288 195631 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
21997225 55783 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162265 55783 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
11738728 18499 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 18499 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
9817774 111497 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL327782 111497 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
1353 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
3559 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
86 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
CHEMBL54 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
DB00502 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
10760638 188176 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 188176 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
56852956 112043 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112043 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
10425969 101008 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294459 101008 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
792460 92146 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420773 92146 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
56852956 112043 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 112043 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
137634397 156105 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 156105 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
10069973 52399 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
CHEMBL159022 52399 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
44369020 119459 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
CHEMBL345111 119459 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
10425450 201 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
17461770 201840 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL60708 201840 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
44370032 47389 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
CHEMBL154482 47389 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
10092819 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
CHEMBL124444 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
10092819 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
11068912 30864 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL139722 30864 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10542345 18880 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128281 18880 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
135398737 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
38 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
722 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
CHEMBL42 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
DB00363 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
10781960 15559 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
CHEMBL121993 15559 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
162671033 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 183755 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
154726793 176233 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4590966 176233 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 176233 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
135398737 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
38 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
722 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
CHEMBL42 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
DB00363 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
2726 919 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
49782602 17169 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256169 17169 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
49782604 17523 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1257927 17523 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
137636351 155873 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 155873 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
73347474 91059 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397478 91059 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
71733935 90983 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 90983 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
122177641 121209 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 121209 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11474021 4794 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104089 4794 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
135398737 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
38 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
722 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
CHEMBL42 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
DB00363 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
53248675 66369 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813594 66369 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851639 66369 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
168293632 193000 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5203856 193000 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222695 193000 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
10092819 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
CHEMBL124444 16773 0 None -28 12 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
11068912 30864 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL139722 30864 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
135398737 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 958 93 None -13 89 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
90644068 112037 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289650 112037 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
10616050 186646 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 186646 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
164621627 185483 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 185483 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
44419053 84287 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
CHEMBL221397 84287 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
44323890 206917 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90977 206917 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
49783039 17653 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
CHEMBL1258383 17653 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
127045855 139664 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139664 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
118709163 113409 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318835 113409 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137655795 158582 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 158582 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
3038495 708 37 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 708 37 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 708 37 None -91 19 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
10917920 111446 0 None -3801 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 111446 0 None -3801 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10404663 166861 10 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL428561 166861 10 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
122189390 123245 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 123245 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
25129807 103294 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL3084502 103294 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
44330640 208301 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99054 208301 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
164619170 185601 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185601 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
168271259 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179459 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
163322331 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5204764 192215 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
11720119 83226 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL218607 83226 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
164619170 185601 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185601 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9888555 165604 16 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 165604 16 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
130431334 174426 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4552939 174426 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
168271259 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179459 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168271259 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 190515 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
53248159 61989 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 61989 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
10098342 137990 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
CHEMBL376445 137990 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
72164300 92155 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420782 92155 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44393415 65230 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182652 65230 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
44336352 111000 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326250 111000 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
9818076 16224 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL122427 16224 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL5286175 194337 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 340 1 1 4 4.0 Clc1ccc2c(c1)N=C(N1CCN(c3ccccc3)CC1)CCN2 10.1016/j.ejmech.2020.113141
164621627 185483 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 185483 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
60167166 75295 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037430 75295 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60167166 75295 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037430 75295 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44431487 88074 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234646 88074 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
137632761 156574 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 156574 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137654675 158634 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 158634 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
137633705 156618 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 156618 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
122181331 121872 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590082 121872 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
10691634 100651 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL292186 100651 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
11793892 198051 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL57407 198051 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273912 78050 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20996 78050 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273897 98708 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277669 98708 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 919 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 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 -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
76325152 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
53248677 66419 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1813595 66419 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1851893 66419 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
127053218 139478 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 139478 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
17469721 78025 5 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL209832 78025 5 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
10359539 59054 10 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169459 59054 10 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
3033769 3281 61 None -562 19 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
3299 3281 61 None -562 19 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
94 3281 61 None -562 19 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
CHEMBL8809 3281 61 None -562 19 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
DB12518 3281 61 None -562 19 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
25139180 184341 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL484357 184341 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
114840 69583 59 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL19344 69583 59 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL5079053 214601 0 None -107 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CC(=O)N2CCC(c3ccccc3)(c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c00611
9926141 170256 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
CHEMBL444596 170256 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
11442138 69189 0 None -75 3 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL192650 69189 0 None -75 3 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
10470579 207374 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93753 207374 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
155195487 173276 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 173276 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
9816808 206310 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL87137 206310 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
49783419 17749 0 None -151 12 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 17749 0 None -151 12 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
130431277 169932 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4441358 169932 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
44376920 55355 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161899 55355 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44273925 77294 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20819 77294 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
44273815 78135 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21035 78135 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
168268918 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5171398 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
137636308 156202 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 156202 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
10430685 54299 0 None -107 5 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
CHEMBL160817 54299 0 None -107 5 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
6466372 170062 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
53248256 62035 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
CHEMBL1774536 62035 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
44438239 154934 2 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL401031 154934 2 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
168268918 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5171398 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
168268918 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 190007 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
15290395 99899 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28605 99899 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
44278829 100477 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29087 100477 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10065188 101604 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 101604 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
135398737 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 958 93 None -7 89 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
2865 4143 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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
9905720 167933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
CHEMBL431479 167933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
10704110 115741 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL335392 115741 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
16094699 82145 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 82145 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
72544787 93130 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 93130 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137644966 158494 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 158494 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
21219160 92007 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24170 92007 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10014924 107271 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 107271 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 107271 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 107271 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
11383473 4880 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL104431 4880 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
11393899 4891 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104485 4891 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11360382 5044 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105234 5044 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11795245 111703 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL2112375 111703 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL328681 111703 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
57394285 70458 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946125 70458 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
11151920 80034 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 80034 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
76325152 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 106371 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
109030343 170860 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170860 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10065188 101604 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 101604 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
49788940 18273 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270422 18273 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10424961 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL544184 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL91350 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10424961 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL544184 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91350 206980 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL5283608 194220 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 345 6 0 6 3.0 CCOC(=O)c1nn(-c2ccccc2)cc1CN(C)[C@@H]1CCSC1 10.1016/j.ejmech.2020.113141
CHEMBL5280960 194090 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 336 5 0 5 3.2 Cc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)n1 10.1016/j.ejmech.2022.114840
9980998 31035 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 31035 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 31035 0 None -1148 8 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44538690 109851 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233432 109851 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
72737750 114523 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 114523 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
137640152 156753 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4070604 156753 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
155514430 169864 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4440301 169864 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
168270455 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
155195501 170093 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
CHEMBL4443441 170093 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
168270455 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5171772 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168270455 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5171772 190033 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5280960 194090 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 336 5 0 5 3.2 Cc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)n1 10.1016/j.ejmech.2022.114840
44355433 22179 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
CHEMBL132261 22179 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
10642702 39210 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL147003 39210 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
12997413 7128 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108527 7128 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
44431494 148750 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL394042 148750 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
154725389 176648 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4453405 176648 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4598003 176648 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
3198 205513 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
122180569 121721 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588914 121721 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
44431459 87322 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL233214 87322 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
53248361 62082 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
CHEMBL1774991 62082 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
10782049 20026 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130347 20026 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155515759 170005 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4442419 170005 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
109030515 175985 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175985 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25070419 111778 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287394 111778 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
44405414 71820 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL196866 71820 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
11678172 78032 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 78032 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
118709160 113406 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318832 113406 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709173 113421 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318846 113421 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
22727324 13428 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1192902 13428 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544220 13428 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
681 1465 72 None -2 39 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1465 72 None -2 39 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1465 72 None -2 39 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1465 72 None -2 39 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1465 72 None -2 39 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
9975465 187651 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 187651 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10086123 111484 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL327713 111484 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
72205045 91946 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414356 91946 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
44436606 91997 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241641 91997 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
102262219 140059 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 140059 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
15508238 4795 1 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
CHEMBL104092 4795 1 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
44319370 107047 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 107047 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
134156222 154351 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 154351 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
44283889 120121 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL35114 120121 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
134156222 154351 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 154351 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
130431337 174087 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4544583 174087 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44336052 5434 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL107351 5434 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
10801405 26407 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL135944 26407 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44393403 65078 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 65078 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
53248213 62034 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 62034 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
164627741 186505 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4877460 186505 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
71062708 154306 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 154306 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168294968 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168294968 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5208124 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168294968 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5208124 192419 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL5092747 215385 0 None -16 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
CHEMBL5092747 215385 0 None -16 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
25895957 4844 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104251 4844 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
10641954 206931 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
CHEMBL91067 206931 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
10335148 78886 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112912 78886 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
21465540 111415 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327310 111415 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
2946349 99733 7 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL284892 99733 7 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
9975465 187651 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 187651 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
10641954 206931 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91067 206931 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1016/j.ejmech.2020.113034
44403210 70543 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194727 70543 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
10137748 53061 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL159742 53061 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
71652196 87454 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL2333732 87454 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
191 403 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
201 403 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
2170 403 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
CHEMBL1113 403 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
DB00543 403 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
44431481 88035 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234472 88035 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137643951 158259 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 158259 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
16105549 67785 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL1908879 67785 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL221640 67785 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
122181330 121871 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121871 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833378 68333 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 68333 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
44276050 13280 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191675 13280 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542809 13280 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
22727331 13327 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1192096 13327 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL543278 13327 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
44438228 93556 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 93556 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
19958494 99453 1 None 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
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 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
127052467 140851 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140851 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
44381117 57831 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167032 57831 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
72545010 93125 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 93125 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
44319102 206141 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 206141 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
10276451 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 200285 37 None -2754 10 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
45483654 198118 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
CHEMBL574569 198118 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
135545150 38472 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146410 38472 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
71658076 90402 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386615 90402 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
60165539 75352 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037524 75352 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5075990 214407 0 None -31 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
168291477 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5199649 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
168291477 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
42626318 56236 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627306 56236 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
49799693 14395 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173366 14395 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200278 14395 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
11144835 119693 0 None -114 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL347290 119693 0 None -114 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
127051843 140751 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140751 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44395714 12865 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL1188714 12865 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537182 12865 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
11849181 80060 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 80060 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
60165411 75357 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037529 75357 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
22727356 13326 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1192095 13326 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543277 13326 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
168291477 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5199649 191881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
127051843 140751 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 140751 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44438220 93450 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246021 93450 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
12066265 97111 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL267562 97111 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
44339953 109700 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109700 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
10436653 32792 1 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
CHEMBL141419 32792 1 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
127031500 139350 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 139350 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
71460561 81822 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164346 81822 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
127052467 140851 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 140851 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
57391306 70159 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940407 70159 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
90644227 111780 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111780 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
44436617 91560 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL240584 91560 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
11176211 4791 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
CHEMBL104079 4791 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
44283891 120190 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35182 120190 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
90644059 112030 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 112030 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
10714184 78602 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112284 78602 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
10972865 203728 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL67750 203728 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
71657947 90397 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386610 90397 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
145986441 167172 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4291172 167172 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
12050198 200254 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59702 200254 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
92716 72333 22 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
CHEMBL19844 72333 22 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
44381286 120367 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL353220 120367 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
380039 14308 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169728 14308 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199909 14308 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
44438224 154636 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399396 154636 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180570 121722 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588915 121722 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44438199 151319 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL396092 151319 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5091479 215310 1 None -4 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN1CCC(c2ccccc2)(c2ccccc2)C1 10.1021/acs.jmedchem.1c00611
44330585 208308 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99085 208308 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
130431325 172412 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4476699 172412 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
11809415 120963 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL356171 120963 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11784937 121875 19 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
CHEMBL3590085 121875 19 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
155195496 170716 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 170716 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
10063875 102321 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
CHEMBL303556 102321 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
56675269 66410 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1813585 66410 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1851858 66410 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
44394599 66234 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184551 66234 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
44436301 90632 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238915 90632 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
10472143 119277 0 None -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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
9867004 169268 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL441274 169268 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
155529568 171453 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463276 171453 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155554837 174636 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 174636 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
127031201 139375 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 139375 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031513 139474 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 139474 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
90644059 112030 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 112030 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
16725931 151040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL395867 151040 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122181327 121868 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590078 121868 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
3802 203023 21 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL63329 203023 21 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737723 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
155554837 174636 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 174636 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
76318473 106294 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133868 106294 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139054 106294 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
57393627 69307 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 69307 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709162 113408 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318834 113408 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45270861 195080 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL549638 195080 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11078813 112018 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL328925 112018 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10973768 107560 0 None -9332 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 107560 0 None -9332 9 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10276451 200285 37 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 200285 37 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 200285 37 None -2754 10 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
71086303 160810 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4114493 160810 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168293874 192179 0 None -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 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 -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 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
44426502 142066 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387952 142066 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44309688 203992 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
CHEMBL69571 203992 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
25132869 103295 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 103295 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
44438221 148779 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394065 148779 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122181007 121796 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
CHEMBL3589652 121796 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
6674 2817 26 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
9891901 2817 26 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL300780 2817 26 None -3019 8 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
11812065 204020 7 None -91 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL69717 204020 7 None -91 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL5077645 214509 0 None -97723 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc([C@@]23CCC[C@@H]([C@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1021/acs.jmedchem.1c00611
10403435 13450 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1193072 13450 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL544418 13450 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
9820313 106194 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL313851 106194 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44335896 5376 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106998 5376 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336005 5443 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107391 5443 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
57399494 70457 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 70457 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 175369 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 175369 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
57399494 70457 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
CHEMBL1946124 70457 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
134146195 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
127032084 139341 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 139341 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031830 139432 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 139432 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
10385977 97331 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26929 97331 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431479 87580 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233581 87580 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122189387 123242 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613873 123242 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
71734028 91053 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397390 91053 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
11079832 164913 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL422310 164913 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
44372153 120164 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL351550 120164 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
57399494 70457 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 70457 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 175369 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 175369 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134146195 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 154591 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
139877715 192822 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5179879 192822 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221531 192822 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
9906454 138271 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL37706 138271 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
10939408 47423 0 None -645 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
CHEMBL154508 47423 0 None -645 6 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
12050197 100874 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL293645 100874 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
12049521 203191 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64288 203191 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44381276 58728 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168541 58728 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
3228 3146 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
9909448 3146 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
CHEMBL71838 3146 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
10086348 8052 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
CHEMBL109101 8052 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
10086348 8052 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
CHEMBL109101 8052 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
164619127 185525 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185525 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
71657943 90393 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386606 90393 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
10254390 71688 0 None -2884 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
CHEMBL196476 71688 0 None -2884 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
164619127 185525 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185525 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
168277394 190401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 190401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
6917970 3691 61 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 3691 61 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 3691 61 None -851 34 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
11477180 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
6675 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
CHEMBL180010 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
11778580 66127 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 66127 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
11477180 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
6675 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
CHEMBL180010 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
11477180 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
6675 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
CHEMBL180010 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
11477180 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
6675 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL180010 3074 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
44438203 93655 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246848 93655 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
17756213 149704 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 149704 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
11300847 204990 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL76653 204990 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
154706431 176585 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4531363 176585 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 176585 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49798833 14360 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172212 14360 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200152 14360 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL5073754 214305 0 None -15 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11716449 141215 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 141215 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
4420454 56259 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 56259 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10548105 18870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL128222 18870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
11256262 80001 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 80001 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
56837636 69297 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 69297 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
127046952 140101 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 140101 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
10548105 18870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128222 18870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
11199162 79859 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 79859 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
12899499 66623 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813596 66623 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852734 66623 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL5083473 214865 0 None 5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
3038495 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
7625 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
CHEMBL25236 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
4420454 56259 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 56259 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
11615489 69443 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL193337 69443 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
10039198 56349 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56349 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL5072449 214281 0 None -8 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
90389592 147674 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3931765 147674 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389592 147674 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3931765 147674 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
154705520 176260 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4452683 176260 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 176260 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
71455083 81830 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81830 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
53325242 57070 0 None -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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 -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
9907381 4897 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104514 4897 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
72191064 92359 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430442 92359 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44438211 147462 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL393027 147462 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
54477 84653 36 None -14 23 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
CHEMBL22242 84653 36 None -14 23 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
3038495 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
2865 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
103 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2865 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 4143 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
103 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
57394810 70157 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940405 70157 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
49782601 17488 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1257810 17488 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
45267409 196161 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL561262 196161 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
9906895 119956 2 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349699 119956 2 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
12050202 203298 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64752 203298 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
45379369 7522 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 7522 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
8592415 65169 6 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 65169 6 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10477871 83230 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218638 83230 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
11570589 84249 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL221129 84249 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
4064342 207041 31 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91621 207041 31 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
12050199 100812 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL293225 100812 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44304652 200322 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 200322 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
44319368 106064 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 106064 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
10824155 57240 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL165022 57240 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
164622629 185596 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4863748 185596 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
10885524 103126 0 None -38 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL307800 103126 0 None -38 5 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
10572985 163482 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL420067 163482 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
1016 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
71061611 149060 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3942898 149060 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
155522719 170790 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4453069 170790 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
135404757 120958 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL356149 120958 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
44438213 93409 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245815 93409 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44438223 93492 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246231 93492 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5077104 214481 0 None -64 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCC(=O)N1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
70788951 27155 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 27155 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72191065 92358 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
CHEMBL2430441 92358 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
118719798 115725 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353901 115725 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44356253 11578 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180604 11578 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL134808 11578 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
46231784 201338 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 201338 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11762743 103814 0 None -109 5 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL309118 103814 0 None -109 5 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
44394884 122659 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL360394 122659 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
9951233 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL305276 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
10045525 203781 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL68191 203781 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
44264682 97318 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
CHEMBL269202 97318 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
11724450 123848 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 123848 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 123848 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
9951233 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/j.ejmech.2020.113141
CHEMBL305276 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/j.ejmech.2020.113141
9799781 120204 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL351963 120204 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/j.ejmech.2020.113141
10430183 205628 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 205628 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
44335995 108464 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL319923 108464 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336000 108988 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321201 108988 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44336050 5314 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
CHEMBL106742 5314 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
9800164 4952 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104788 4952 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335796 4965 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104832 4965 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
9799781 120204 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351963 120204 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
10045525 203781 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL68191 203781 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
10543298 39855 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
CHEMBL147731 39855 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
10567507 119260 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL343657 119260 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
60165416 75296 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037431 75296 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165416 75296 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037431 75296 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44405492 140522 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL381019 140522 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
11638780 77095 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL207488 77095 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10044835 111406 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL327245 111406 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
9951233 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
CHEMBL305276 102790 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
54583898 61611 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771114 61611 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44376569 57441 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 57441 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
168286048 192922 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5191408 192922 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5222229 192922 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
57396484 70169 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940417 70169 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396484 70169 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940417 70169 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
56926585 69005 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923293 69005 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
10090130 192993 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5199358 192993 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222630 192993 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
44340097 9440 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9440 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10759511 206964 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL91273 206964 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
4826074 104104 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 104104 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
9902381 119511 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL345552 119511 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
9885114 119604 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 119604 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
1353 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
3559 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
86 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
CHEMBL54 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
DB00502 1911 93 None -3 83 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
10759511 206964 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91273 206964 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
9887091 107389 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL317879 107389 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10023466 164914 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
CHEMBL422314 164914 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
CHEMBL5290993 194519 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 301 2 1 2 3.0 CC(C)N1C[C@H](NC(=O)N2Cc3ccccc3[C@@H]2C)[C@@H](C)C1 10.1016/j.ejmech.2020.113141
9885114 119604 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1016/j.ejmech.2020.113141
CHEMBL346389 119604 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1016/j.ejmech.2020.113141
21527771 70156 1 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 70156 1 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
25139181 184342 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 184342 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
25072941 156474 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 156474 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
10780942 21331 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL131396 21331 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
10805355 22400 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132455 22400 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
118719926 115780 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 115780 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
10719212 207254 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
CHEMBL92924 207254 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
72164299 92153 5 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420780 92153 5 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
10780942 21331 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL131396 21331 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10805355 22400 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132455 22400 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10519543 113497 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL332001 113497 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155519378 170411 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4448166 170411 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
25072632 111776 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 111776 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
18403576 6191 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL108122 6191 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
71294321 192786 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172871 192786 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221357 192786 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
10593869 207028 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91553 207028 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10574303 207320 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93432 207320 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
11451022 92156 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420890 92156 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
6603950 203324 9 None -7 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 203324 9 None -7 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
3050372 70166 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940414 70166 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
127047996 139646 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139646 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
71583848 87731 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87731 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
11315028 110644 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL325789 110644 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
155529592 171447 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463200 171447 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71454294 84077 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 84077 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44340084 9088 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9088 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10549355 205503 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80722 205503 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
9948965 115369 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL334989 115369 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
137633863 156625 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156625 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44459463 99159 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL281195 99159 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10020040 99968 0 None 9 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28651 99968 0 None 9 3 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
155528865 171389 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 171389 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
155528865 171389 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 171389 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
137660046 159343 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 159343 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
71734129 91061 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397480 91061 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
1613 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
205 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
3964 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
CHEMBL831 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
DB00408 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
1613 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
205 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
3964 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
CHEMBL831 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
DB00408 2348 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
9839426 12150 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1184179 12150 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL337228 12150 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
11153076 4957 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL104801 4957 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
137631542 156411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4066603 156411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
72901200 119777 25 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
CHEMBL3480577 119777 25 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
3626837 207315 11 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
CHEMBL93403 207315 11 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
10862425 116633 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
CHEMBL336930 116633 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
44335678 4810 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104155 4810 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
11058829 168645 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1016/j.ejmech.2020.113141
CHEMBL436274 168645 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1016/j.ejmech.2020.113141
21219166 100072 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL287217 100072 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44436608 146756 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 146756 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
122181332 121873 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121873 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833464 68396 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916720 68396 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
11230330 135187 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 135187 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
11417804 4834 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104216 4834 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11750030 4854 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
CHEMBL104307 4854 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
11058829 168645 0 None 2 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL436274 168645 0 None 2 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
49798837 14344 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1171249 14344 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200077 14344 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10761258 101107 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
CHEMBL295094 101107 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
134130247 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
11036640 121147 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL357684 121147 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
10040546 206705 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL89719 206705 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
155552695 174044 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4543685 174044 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
11407122 167813 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL430658 167813 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
12050201 202874 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL62624 202874 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
42626318 56236 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627306 56236 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
71658205 90406 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386619 90406 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
44438234 93611 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246644 93611 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
16094681 83347 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 83347 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
164609172 184407 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 184407 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
127051592 140878 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140878 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140878 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
56594534 70600 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 70600 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
11036640 121147 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL357684 121147 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10761258 101107 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
CHEMBL295094 101107 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
134130247 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 154575 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
25070742 111782 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
CHEMBL3287398 111782 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
118709178 113348 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3317465 113348 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709161 113407 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318833 113407 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137657322 159643 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4103639 159643 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
164622487 186122 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4871850 186122 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11584858 82772 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL217981 82772 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
155562395 175948 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175948 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
11545813 181194 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476109 181194 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
10617946 205518 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80833 205518 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10805797 112906 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
CHEMBL331045 112906 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
145979855 166528 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4279136 166528 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
44319102 206141 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 206141 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
20354789 114524 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 114524 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
142590702 179796 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4744824 179796 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
22727346 13165 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190866 13165 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541791 13165 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
10597050 109196 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL321557 109196 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
44393372 66326 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL184993 66326 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
127053198 139372 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 139372 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 139483 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 139483 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
56964794 74064 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022272 74064 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
122189393 123248 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 123248 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
46917563 68335 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 68335 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
1353 1911 93 None -3 83 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
3559 1911 93 None -3 83 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
86 1911 93 None -3 83 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
CHEMBL54 1911 93 None -3 83 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
DB00502 1911 93 None -3 83 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
10761912 112317 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL329228 112317 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10810976 207923 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
CHEMBL96799 207923 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
9928335 120097 2 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35093 120097 2 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10520781 206985 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
CHEMBL91367 206985 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
16103 204638 47 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL73538 204638 47 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
1438298 38619 5 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
CHEMBL1465169 38619 5 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
44381146 58507 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168372 58507 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL5087504 215104 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc(C(CCNCCCCN2CCN(c3ccccc3)CC2)c2cccc(O)c2)c1 10.1021/acs.jmedchem.1c00611
17755868 143118 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 143118 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44330650 107402 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317988 107402 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
11676873 9195 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL110365 9195 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
122180612 121740 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588983 121740 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
17755991 152298 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 152298 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL5073904 214307 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL5269361 193599 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 1 4 3.1 Fc1ccc(OC[C@@H]2CN(Cc3ccc4[nH]cnc4c3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
16744004 92328 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL243012 92328 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
72191068 92355 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430438 92355 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL5269361 193599 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 1 4 3.1 Fc1ccc(OC[C@@H]2CN(Cc3ccc4[nH]cnc4c3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
168270563 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170381 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168270563 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168270563 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170381 189950 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
9843137 4827 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104196 4827 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
71657944 90394 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386607 90394 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
49783209 17609 0 None -21 26 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 0 None -21 26 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44335996 4925 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104678 4925 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
9796180 112870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL330966 112870 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
93601125 139351 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 139351 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
44276170 96317 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26135 96317 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
10001519 99309 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28209 99309 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431463 88070 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234641 88070 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
11761412 116951 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 116951 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
72737744 114518 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 114518 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
44408818 140165 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 140165 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
164621388 185736 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 185736 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
11328099 4850 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL104291 4850 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
9826801 107937 0 None -18620 11 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 107937 0 None -18620 11 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
57390694 70466 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946255 70466 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57390694 70466 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946255 70466 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
57403981 70495 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946745 70495 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76524414 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44330639 208175 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98331 208175 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
11488247 200639 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 200639 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
71062664 146861 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL3925231 146861 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
168292271 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5199815 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
76524414 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 140869 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
46231849 201418 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 201418 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
9950913 102752 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
CHEMBL305061 102752 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
11794570 198745 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
CHEMBL58296 198745 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
10884046 165369 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL423735 165369 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44403213 71787 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL196744 71787 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
155531809 171657 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4466114 171657 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
162648426 179960 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
CHEMBL4746695 179960 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
127053215 139424 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 139424 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
164621388 185736 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 185736 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
44431466 88071 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234643 88071 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
11794570 198745 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
CHEMBL58296 198745 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
1248739 140086 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL380054 140086 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
22100962 204267 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71209 204267 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
135398737 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 958 93 None -13 89 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
3038495 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 708 37 None -91 19 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
242 470 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
34 470 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60795 470 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
CHEMBL1112 470 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
DB01238 470 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60165541 75346 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037518 75346 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44329749 112604 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
CHEMBL330216 112604 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
164609650 184997 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 184997 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
10003809 83165 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
CHEMBL218318 83165 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
137653986 158730 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4093493 158730 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
44319369 205819 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 205819 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
168292271 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44381432 120718 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL354748 120718 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
71658208 90409 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386622 90409 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
168292271 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5199815 191889 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
134141355 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44582675 189701 0 None -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 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 -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 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
76318477 106289 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133875 106289 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139049 106289 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
44438226 154663 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399601 154663 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180573 121725 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588918 121725 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
134141355 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 154585 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
168295019 192499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 192499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
44396220 125423 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 125423 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
133633 2241 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
177 2241 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
CHEMBL445102 2241 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
44278496 99549 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28355 99549 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
44278624 100344 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28953 100344 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
52943802 17618 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258270 17618 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57395341 69311 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 69311 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
71583849 87732 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336893 87732 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
164609650 184997 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 184997 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
6937303 203207 7 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64376 203207 7 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
44264742 97174 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
CHEMBL268190 97174 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
75201901 166425 19 None -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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 -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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
42626380 56243 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627313 56243 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
3191 102858 97 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
145986752 167276 0 None -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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 -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
44393403 65078 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182379 65078 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
10432808 58749 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168611 58749 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
10001207 165321 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL423440 165321 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
155514137 169828 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4439728 169828 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
118709179 113426 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318851 113426 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44222488 196226 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
CHEMBL561622 196226 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
11303390 4887 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104476 4887 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
8592415 65169 6 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 65169 6 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10763496 111597 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL328283 111597 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
135471592 121682 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL358657 121682 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737728 114519 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 114519 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
127051592 140878 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 140878 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 140878 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
42606339 17931 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 17931 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
44381279 58739 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168571 58739 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44330638 107277 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317051 107277 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
44335722 108876 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321058 108876 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44427827 93275 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 93275 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
44276105 13454 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193100 13454 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544451 13454 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL5093200 215416 0 None -39 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10546828 205426 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80207 205426 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44323762 206577 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL88837 206577 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
44323851 206974 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91310 206974 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
76309672 85888 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298811 85888 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
45482151 198009 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
CHEMBL573791 198009 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
9843031 110065 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL323537 110065 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
44380815 59010 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169193 59010 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
11299620 97284 3 None -87 6 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL269004 97284 3 None -87 6 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
127032086 139322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 139322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
127030606 139362 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 139362 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
90644226 111779 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111779 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
122181328 121869 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590079 121869 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
135398737 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
38 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
722 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
CHEMBL42 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
DB00363 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
11033734 9721 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL113238 9721 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
164609529 184464 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 184464 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
76336022 106379 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 106379 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 106379 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
11304676 102806 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL305366 102806 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
10587140 205034 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
CHEMBL77015 205034 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
137643132 158050 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 158050 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
164609172 184407 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 184407 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10454026 17907 0 None -1479 9 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL125916 17907 0 None -1479 9 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
168275515 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
168275515 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179340 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168275515 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179340 190505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
2726 919 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
9886340 5414 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL107229 5414 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
44380816 120351 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353090 120351 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
6604756 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL278751 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
6604756 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
CHEMBL278751 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
164609529 184464 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 184464 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
57390116 69298 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 69298 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
11732013 40809 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148559 40809 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
6604756 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL278751 98831 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
72190766 92360 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL2430443 92360 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
10831786 205523 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80863 205523 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
156016177 177654 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
CHEMBL4641502 177654 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
16744005 143878 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL390181 143878 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
46231782 200503 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 200503 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
44415704 80159 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 80159 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
10242548 25604 40 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135152 25604 40 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
118719792 115719 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3353895 115719 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
21171 186976 33 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 186976 33 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
56589561 70601 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 70601 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
13091358 70455 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946122 70455 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
9845181 208161 3 None -34 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 208161 3 None -34 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
13091356 113538 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 113538 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
44276155 99492 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL283211 99492 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
72164180 92145 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420772 92145 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
118709165 113411 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318837 113411 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709167 113413 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318839 113413 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
25141534 56235 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 56235 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
146025727 171685 0 None -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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 -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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
11016418 106122 0 None -7943 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 106122 0 None -7943 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
137645196 157958 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4084712 157958 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
49798855 14310 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169896 14310 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199933 14310 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
10597114 171849 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL446892 171849 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
71061585 160497 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4112090 160497 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4752561 214038 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4
ChEMBL None None None COc1cc(-c2cn([C@H]3CCc4ccccc4N(CC(F)(F)F)C3=O)nn2)ccc1-n1ccc(C)n1 10.6019/CHEMBL5212743
164619236 185709 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 185709 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10551026 101617 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101617 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
9821803 127466 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366043 127466 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
131396 206735 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 206735 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
10641783 42679 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150129 42679 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
9820304 102069 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL1204116 102069 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL302075 102069 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
1353 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
3559 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
86 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
CHEMBL54 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
DB00502 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
44336047 4785 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104058 4785 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335925 4945 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104751 4945 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335835 5075 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105454 5075 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
9867233 5501 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL107631 5501 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
9865490 167949 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL431640 167949 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335795 5001 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105011 5001 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44335816 5217 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106208 5217 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
10157556 120235 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 120235 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
127031515 139434 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL3793910 139434 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
1353 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 1911 93 None -3 83 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
11668034 133527 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370823 133527 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
22100940 203954 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL69355 203954 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
19958507 99421 0 None 81 5 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
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 81 5 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10715375 199701 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59326 199701 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
10525119 79739 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21168 79739 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
127031515 139434 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL3793910 139434 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
76325156 106390 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 106390 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 106390 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
10049549 83266 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
CHEMBL218787 83266 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
9968343 42739 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL150181 42739 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
155563452 175309 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 175309 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
145967572 164933 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 164933 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
72545238 93127 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 93127 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
155563452 175309 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 175309 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
10643589 207468 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94283 207468 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3691783 4764 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL103871 4764 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
11797442 107026 0 None 6 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL315446 107026 0 None 6 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
127031832 139415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 139415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
16759175 54994 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1334895 54994 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1616116 54994 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
137651073 157468 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 157468 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
10360923 91551 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24052 91551 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
10737474 101353 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 101353 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
9975465 187651 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 187651 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
137661377 159209 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 159209 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
44412191 138375 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
CHEMBL377200 138375 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
10737474 101353 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 101353 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
13091268 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL210578 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
13091268 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
13091268 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL210578 78224 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
25071691 111787 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111787 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
44412191 138375 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
CHEMBL377200 138375 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
71734031 91060 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397479 91060 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
10133031 57538 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166321 57538 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
10518406 18878 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128276 18878 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10518406 18878 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128276 18878 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
9952003 5360 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 5360 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10000302 207221 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL92713 207221 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
127031831 139340 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 139340 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
11504230 78217 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 78217 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
53364153 63841 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803023 63841 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
11233944 4783 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104041 4783 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10000302 207221 0 None 109 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92713 207221 0 None 109 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10760638 188176 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 188176 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
57396571 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
10618874 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL6416 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10667201 111392 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327176 111392 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
10546453 111702 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328667 111702 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10760638 188176 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49876 188176 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
10618874 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
CHEMBL6416 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
168280742 191084 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 191084 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
145969667 164965 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164965 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
10618874 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
CHEMBL6416 203146 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
11774177 5383 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107068 5383 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL4513786 213967 7 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL4796803 213967 7 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
10693793 107701 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL319079 107701 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10758004 21411 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL131484 21411 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
57396571 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396571 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940413 70165 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
19964410 159698 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4104272 159698 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
10758004 21411 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131484 21411 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
6466372 170062 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 170062 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
15467371 101007 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294458 101007 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
45482152 198010 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
CHEMBL573792 198010 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
57401706 70171 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 70171 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401706 70171 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940419 70171 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
25071692 111789 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111789 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
76325156 106390 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 106390 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 106390 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
44364166 40813 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
CHEMBL148561 40813 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
9926143 113526 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 113526 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
127031515 139434 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 139434 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
145969667 164965 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164965 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
52919 14450 48 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL1200986 14450 48 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
71733932 91052 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2397389 91052 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10378194 197765 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 197765 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
155523515 170865 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4454096 170865 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155555060 174325 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
CHEMBL4550633 174325 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
44278479 163142 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL417858 163142 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
135887934 11332 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179502 11332 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80627 11332 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10084583 104778 4 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104778 4 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10639430 169169 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL440511 169169 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
135398745 2914 112 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
44454707 97831 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL272073 97831 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44335987 4813 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104160 4813 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
132578545 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
135398745 2914 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
47 2914 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
CHEMBL715 2914 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
DB00334 2914 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
10663221 33713 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
CHEMBL142217 33713 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
22727323 13141 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1190607 13141 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL541270 13141 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
44270444 49324 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL156369 49324 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
44273882 78228 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21059 78228 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
10939222 204402 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL71960 204402 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
132578545 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 154558 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
2865 4143 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
44340415 8578 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8578 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340302 9752 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9752 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44332686 208424 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL99849 208424 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL5267339 193520 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 340 5 1 5 3.1 Clc1ccc(-n2cc(CNC[C@@H]3CCCOC3)nn2)c(Cl)c1 10.1016/j.ejmech.2020.113141
130431290 174035 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
CHEMBL4543524 174035 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
72545009 93124 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 93124 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
11659604 138574 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL377542 138574 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
10034684 69407 69 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 69407 69 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155568411 176080 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 176080 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
137647533 157953 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4084690 157953 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11154555 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
164619236 185709 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 185709 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
154704705 176325 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4590356 176325 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 176325 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL5074399 214316 0 None -19 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
130431336 174908 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4564507 174908 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
71062579 148230 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
CHEMBL3936182 148230 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
44427970 152610 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 152610 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
11269330 201493 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 201493 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44330637 208174 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98330 208174 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
11154555 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 800 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
16744171 92557 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243224 92557 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
57345620 70494 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946744 70494 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76518515 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
13373172 199783 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 199783 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
44335721 107303 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL317266 107303 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
127030909 139481 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 139481 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
57402787 69195 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 69195 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
44276111 12910 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189040 12910 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL537975 12910 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
10247720 13054 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 13054 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 13054 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
60165543 75347 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037519 75347 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
9881815 206668 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL89420 206668 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
242 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
34 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
60795 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
CHEMBL1112 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
DB01238 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
122180574 121726 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588919 121726 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
154725277 176432 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4472900 176432 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 176432 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
242 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr 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.2021.113243
34 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr 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.2021.113243
60795 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr 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.2021.113243
CHEMBL1112 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr 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.2021.113243
DB01238 470 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr 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.2021.113243
242 470 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 470 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 470 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 470 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 470 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
135501649 119766 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL347959 119766 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
71449034 78423 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111526 78423 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
60165545 75355 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037527 75355 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
76518515 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 140870 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44456400 12834 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12834 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12834 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12834 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
44591088 189582 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514591 189582 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44438236 154900 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL400827 154900 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
100 3805 58 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -8 55 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10806501 205283 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL79098 205283 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
9857248 205104 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 205104 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44278458 99690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL28458 99690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
136072267 13173 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1190896 13173 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL541826 13173 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
23992579 92144 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420771 92144 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
3251 4072 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
5684 4072 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
80 4072 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL31354 4072 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44405445 135777 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL373032 135777 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
11280787 109216 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL321701 109216 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12899569 66624 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813597 66624 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852735 66624 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
11375068 161858 1 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
CHEMBL414838 161858 1 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
44578446 181580 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476934 181580 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
118709164 113410 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318836 113410 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44335998 6465 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108261 6465 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657945 90395 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386608 90395 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
109030515 175985 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 175985 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10803828 11583 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180609 11583 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135044 11583 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
130431340 171345 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4461461 171345 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
130431342 169584 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4436025 169584 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
12050200 102090 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL302186 102090 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
2 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
2 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3261 23 None -2 29 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
11772242 166287 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 166287 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
49799687 14391 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173285 14391 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200269 14391 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
135398737 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
44340186 9660 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9660 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
11005852 203868 0 None -263 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL68720 203868 0 None -263 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
72191066 92357 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430440 92357 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
53248209 61991 4 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
CHEMBL1774386 61991 4 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
4189 206922 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
71061785 160496 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL4112056 160496 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10039198 56349 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56349 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
135398737 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -13 89 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -13 89 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -13 89 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -13 89 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
1240 8823 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL109684 8823 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL1256754 8823 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
10403092 25132 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134747 25132 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
145968810 165038 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 165038 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
44431478 87579 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233580 87579 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137657153 159557 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 159557 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
135398737 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 958 93 None -13 89 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
10425450 201 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 201 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 201 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
44393775 66304 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 66304 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
57393634 69319 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 69319 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
127045854 139564 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139564 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44337725 108538 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
CHEMBL320114 108538 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
22727334 12946 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189290 12946 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL538474 12946 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
44455426 155149 0 None -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 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 -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 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
10402378 66125 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 66125 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL5080654 214698 0 None -8709 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1021/acs.jmedchem.1c00611
44336127 109281 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321871 109281 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71455083 81830 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 81830 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
10873318 45547 0 None -12 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152869 45547 0 None -12 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
2407 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
59227 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
941 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
CHEMBL1303 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
DB05271 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
127047859 140051 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 140051 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137635685 156005 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 156005 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
44326256 168136 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL433002 168136 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
44393411 66093 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL183871 66093 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
71455082 81828 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164352 81828 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
11477180 3074 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
6675 3074 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL180010 3074 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
857428 31822 32 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
CHEMBL1406529 31822 32 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
107930 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
130431316 170681 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4451683 170681 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
107930 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 1529 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
71062560 153428 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
CHEMBL3979116 153428 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
154703541 176299 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4541924 176299 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 176299 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1164 1630 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
1626 1630 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
3345 1630 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL596 1630 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
DB00813 1630 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL5279686 194035 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 358 5 0 7 2.6 Cc1csc(OC[C@@H]2CN(Cc3ccc4c(cnn4C)c3)CCO2)n1 10.1016/j.ejmech.2022.114840
9842859 205455 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
CHEMBL80411 205455 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
1621 2429 17 None -64 45 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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
22065962 176796 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
CHEMBL460644 176796 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
132075278 162644 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 162644 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
11036641 31778 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 31778 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71462265 81829 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164353 81829 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
145989012 167306 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
CHEMBL4293886 167306 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
137654511 158803 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4094407 158803 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5279686 194035 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 358 5 0 7 2.6 Cc1csc(OC[C@@H]2CN(Cc3ccc4c(cnn4C)c3)CCO2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5075014 214354 0 None -5 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
76311271 106288 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133862 106288 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139046 106288 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
11646648 93700 8 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
CHEMBL247058 93700 8 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
681 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
763194 92143 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420770 92143 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
164609519 184451 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 184451 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
25071384 111781 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111781 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
242 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
34 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
60795 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL1112 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
DB01238 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
242 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
34 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
60795 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
CHEMBL1112 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
DB01238 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
44419060 137857 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
CHEMBL376020 137857 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
10684789 9212 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL110489 9212 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
30438 198152 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
CHEMBL57478 198152 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
30438 198152 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
CHEMBL57478 198152 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
107995 97126 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
29982233 97126 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
CHEMBL267723 97126 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
118709169 113416 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318841 113416 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10917953 207988 0 None -16595 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 207988 0 None -16595 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
134154069 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
9980998 31035 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 31035 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 31035 0 None -1148 8 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44335948 167925 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL431437 167925 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
154726353 176323 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4577162 176323 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 176323 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
154726792 176584 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 176584 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 176584 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
10684789 9212 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL110489 9212 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
134154069 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 154447 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
168287735 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5198353 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164617626 185460 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 185460 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
164617626 185460 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 185460 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
53324045 57071 0 None -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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 -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
22727332 13743 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1195194 13743 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL554016 13743 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11615489 69443 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 69443 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11356479 71837 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 71837 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
168287735 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5198353 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168287735 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 191804 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
135995891 202960 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62996 202960 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44456400 12834 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 12834 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 12834 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 12834 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
16759249 10007 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
CHEMBL11493 10007 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
44591087 175750 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL458342 175750 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
11464115 68634 0 None -30 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL191815 68634 0 None -30 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
122180576 121728 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588921 121728 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
46231925 201378 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 201378 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
121304441 152384 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 152384 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL5090215 215249 0 None -389 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44339984 167797 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167797 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44370009 49977 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
CHEMBL156896 49977 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
3428803 100490 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29098 100490 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
44307552 102341 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
CHEMBL303692 102341 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
44336085 5179 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106007 5179 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
9840797 15540 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121884 15540 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
127027237 139386 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 139386 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
137657951 159564 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4102646 159564 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
73353534 91058 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397477 91058 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
52937776 61170 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765629 61170 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
44307552 102341 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL303692 102341 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
42606573 17846 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 17846 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
12050196 203118 6 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64043 203118 6 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
12050193 203196 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64325 203196 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
46231846 201339 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 201339 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10735463 161876 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
CHEMBL415014 161876 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
44335877 4860 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104323 4860 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
44336027 5106 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105601 5106 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
44335960 6528 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108282 6528 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336108 5684 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107793 5684 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335923 109193 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL321538 109193 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335884 163377 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419356 163377 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335799 163454 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419908 163454 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
25071691 111787 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111787 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL4547253 213996 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Fc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL4567314 214015 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Brc1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
71459761 84080 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 84080 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10570563 18030 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL1202212 18030 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL126429 18030 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
9836900 41700 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL149233 41700 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
44336012 109214 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321698 109214 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
90644058 112029 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 112029 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
54585811 61610 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771113 61610 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
90644058 112029 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 112029 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
2389 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
72164302 92161 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420895 92161 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
155562328 175843 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4585384 175843 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
57393083 70167 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 70167 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57393083 70167 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940415 70167 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
681 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
940 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
947 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
CHEMBL59 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
DB00988 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
19964401 156646 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4069306 156646 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
11849778 81142 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 81142 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
9817253 106555 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL314174 106555 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
10249755 168184 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL433255 168184 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
15443 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
11336814 80101 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 80101 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11200205 138911 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 138911 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
53363200 63853 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803052 63853 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
16121920 195875 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL558838 195875 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
45267435 195991 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
CHEMBL559868 195991 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
10088259 101913 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 101913 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
71458040 78887 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112913 78887 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
10088259 101913 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 101913 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
155561496 175672 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
CHEMBL4581645 175672 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
10065083 32103 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL140872 32103 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
137638973 156874 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156874 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10065083 32103 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL140872 32103 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
11653679 181191 1 None 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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
168273039 192796 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175009 192796 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221414 192796 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
10498196 41982 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL149497 41982 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
10382581 101298 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 101298 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
15443 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 117810 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
44278114 100205 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
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 104 4 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10382581 101298 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 101298 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
133079 3638 42 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
980 3638 42 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
CHEMBL69759 3638 42 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
11465618 102398 23 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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 -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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 -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 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
53364225 63845 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803027 63845 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
10336538 1625 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 1625 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 1625 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
155562395 175948 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 175948 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
9946469 44122 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL151533 44122 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
9907332 16396 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 16396 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
57391307 70163 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 70163 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391307 70163 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940411 70163 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
168277064 192838 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 192838 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 192838 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10786367 205176 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL78287 205176 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
10018480 13830 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195797 13830 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL555362 13830 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
135398737 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
38 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
722 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
CHEMBL42 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
DB00363 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
135398737 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
38 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
722 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
CHEMBL42 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
DB00363 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
137636066 156233 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 156233 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
71733932 91052 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 91052 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
13457126 99823 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL285543 99823 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
69432471 109846 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233427 109846 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
17755867 86109 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 86109 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
46912547 14392 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173287 14392 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200270 14392 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
164628178 186347 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186347 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
10007017 83028 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
CHEMBL218150 83028 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
12581154 25479 12 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135048 25479 12 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
10184153 13304 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191883 13304 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543041 13304 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
10994141 44924 0 None -831 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
CHEMBL152304 44924 0 None -831 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
164628178 186347 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186347 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
71657942 90392 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386605 90392 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
168268877 189970 0 None -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 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 -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 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
44438204 93656 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246849 93656 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10786591 206729 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
CHEMBL89913 206729 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
3746693 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL61080 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10786591 206729 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL89913 206729 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
3746693 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
CHEMBL61080 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
155538028 172359 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4475978 172359 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
49782603 17489 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257811 17489 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
3746693 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
CHEMBL61080 202402 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
11187628 4872 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104378 4872 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11164922 5378 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
CHEMBL107019 5378 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
9925730 206298 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87067 206298 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
178078 121117 4 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
CHEMBL357416 121117 4 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
8704110 66601 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 66601 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
44340302 9752 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9752 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25139331 169928 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL444128 169928 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
137636298 156198 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4064191 156198 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
681 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1465 72 None -2 39 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
137643122 158035 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 158035 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
10642106 39223 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147011 39223 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
49799715 14333 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170879 14333 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200020 14333 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
44374648 119972 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL349843 119972 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
176 398 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44336105 4936 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104713 4936 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
155195486 169687 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 169687 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
46231847 200574 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 200574 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10544707 16301 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
CHEMBL122531 16301 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
44426509 85743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229024 85743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
242 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 470 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
10357869 4884 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL104453 4884 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
44273920 73924 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
CHEMBL20204 73924 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
44273921 77362 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20854 77362 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
4302960 101061 63 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL294747 101061 63 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
168268735 192769 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5171721 192769 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221227 192769 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5092243 215354 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(OC)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
10430816 168247 1 None -371 4 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
CHEMBL433741 168247 1 None -371 4 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
49788868 18223 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
CHEMBL1270120 18223 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
44437896 152468 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397103 152468 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
10479822 83029 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
CHEMBL218151 83029 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
90389439 145699 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3916231 145699 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389439 145699 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3916231 145699 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
52937871 61172 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
CHEMBL1765631 61172 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
12280575 10287 4 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL11615 10287 4 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
49798797 14356 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172208 14356 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200149 14356 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
3038495 708 37 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 708 37 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 708 37 None -91 19 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
72190766 92360 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430443 92360 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44336175 108197 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL319650 108197 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44339879 172282 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 172282 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
10871118 206807 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
CHEMBL90374 206807 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
44335847 5061 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105354 5061 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
155536022 172103 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4472580 172103 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
164614709 185209 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 185209 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
57400556 69310 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 69310 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
56589560 70597 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 70597 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
164614709 185209 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 185209 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
164621610 186191 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 186191 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL5088070 215136 0 None -75 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
24810004 16550 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12375 16550 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
42626103 56253 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 56253 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
168274755 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5181334 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168274755 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10039198 56349 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 56349 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
11049209 207405 0 None -13182 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL93923 207405 0 None -13182 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11658914 70240 1 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 70240 1 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
54456 162490 28 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
CHEMBL416732 162490 28 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
155568867 176154 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 176154 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
71658206 90407 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386620 90407 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
11316709 168370 0 None -77 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL434532 168370 0 None -77 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
168274850 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5173767 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
168274755 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5181334 190642 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
10761828 38675 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL146557 38675 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
168274850 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5173767 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
168274850 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 190155 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
2993172 127167 4 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 127167 4 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
9828632 100070 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
CHEMBL287198 100070 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
763343 92141 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420769 92141 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
10137747 120173 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL351612 120173 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
164621610 186191 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 186191 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11676195 195148 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 195148 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
72737730 114526 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 114526 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
155535272 172031 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4471669 172031 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
60165535 75350 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037522 75350 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
11428005 5057 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL105312 5057 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
44304643 203275 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64668 203275 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11028157 202721 0 None -128 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
CHEMBL61789 202721 0 None -128 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
30982708 10682 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170683 10682 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
71658203 90404 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386617 90404 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
11247757 133579 0 None -70 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL371200 133579 0 None -70 3 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
44431465 150737 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL395631 150737 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
137645574 157803 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 157803 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
45271691 195553 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL554692 195553 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
45272580 196456 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563109 196456 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
145993700 167330 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294279 167330 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
56833379 68334 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1916550 68334 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL5089932 215233 0 None -25 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
46227273 199811 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
CHEMBL594127 199811 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
155195487 173276 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 173276 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
49799709 14406 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173711 14406 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200302 14406 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
44361021 118786 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
CHEMBL342060 118786 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
44335971 5317 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106751 5317 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10740969 99086 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28063 99086 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
11849267 79872 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 79872 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
127052488 140799 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 140799 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
11133602 30775 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL139600 30775 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
44361021 118786 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
CHEMBL342060 118786 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
45361874 170021 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 170021 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25139481 184840 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
CHEMBL485227 184840 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
154706590 176309 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4590839 176309 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4595264 176309 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
127049061 140767 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 140767 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL5081136 214725 0 None -309 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2C[C@@H](OCCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CN2)c1O 10.1021/acs.jmedchem.1c00611
155516042 176293 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 176293 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 176293 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
154703875 176448 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 176448 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 176448 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10827222 6985 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL108463 6985 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
127049061 140767 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 140767 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
44438231 93609 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246642 93609 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10927750 7378 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108637 7378 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
44438208 93370 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL245614 93370 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
11133602 30775 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL139600 30775 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10713620 39393 1 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
CHEMBL147159 39393 1 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
127052488 140799 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 140799 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
57390118 69302 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 69302 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
22100970 102825 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL305481 102825 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10073022 86058 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL2308105 86058 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
72545008 93123 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 93123 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
10960333 206984 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL91362 206984 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10827222 6985 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 6985 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
44275820 13967 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196753 13967 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL558036 13967 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
44123782 189600 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514747 189600 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
71456889 81824 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164348 81824 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44431476 87577 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233578 87577 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
25139477 184245 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL483593 184245 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44436618 147923 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL393365 147923 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
130442572 171908 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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
130442480 175270 0 None -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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 -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 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
2812 4779 101 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44340333 9662 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9662 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
21462980 47135 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
CHEMBL154286 47135 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
2389 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
5073 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
96 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
CHEMBL85 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
DB00734 3331 118 None -22 67 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
9861459 164118 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL420986 164118 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
6469918 79891 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
CHEMBL212370 79891 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
10646834 107164 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL316317 107164 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
44336099 110688 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326010 110688 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
44336051 111306 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL326670 111306 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
44335798 4845 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104256 4845 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
44335924 4915 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104614 4915 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335886 4940 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104719 4940 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335991 4956 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104800 4956 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
3559 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
86 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
CHEMBL54 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
DB00502 1911 93 None -3 83 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
44405522 71929 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL197225 71929 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
6469918 79891 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79891 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
11338828 5035 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL105181 5035 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
9820680 206204 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL86504 206204 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
681 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 1465 72 None -2 39 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
71151588 118258 0 None -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
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 -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
25071385 159157 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 159157 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
133079 3638 42 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
980 3638 42 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
CHEMBL69759 3638 42 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
2563 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
55 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
91273 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
CHEMBL274047 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
DB12833 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
53361302 63850 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803049 63850 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
53361302 63850 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1803049 63850 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
1353 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
3559 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
86 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
CHEMBL54 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
DB00502 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
1353 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
1353 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
3559 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
86 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
CHEMBL54 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
DB00502 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
10905940 45202 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152576 45202 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
56926586 69009 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923415 69009 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44339953 109700 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109700 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
72164181 92147 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420774 92147 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
127027905 139456 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 139456 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
3069135 70164 3 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940412 70164 3 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
10687362 106607 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL314285 106607 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
10570898 206495 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
CHEMBL88296 206495 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
10687362 106607 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL314285 106607 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
10833953 31125 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140006 31125 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
11811640 165266 0 None 6 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL423040 165266 0 None 6 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
44395741 181581 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL476935 181581 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL558392 181581 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
44372009 48839 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL155913 48839 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10593191 189108 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 189108 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
10593191 189108 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 189108 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
2402 3370 62 None -2 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 3370 62 None -2 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 3370 62 None -2 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 3370 62 None -2 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 3370 62 None -2 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
9798466 134278 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
CHEMBL37170 134278 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
57401819 70160 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 70160 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401819 70160 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940408 70160 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
137657115 159755 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159755 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
9798466 134278 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37170 134278 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10568805 169167 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
CHEMBL440506 169167 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
10568805 169167 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL440506 169167 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
164620912 185735 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4866053 185735 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
137640371 156814 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156814 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
1353 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 1911 93 None -3 83 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
44273908 76716 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20655 76716 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
44273887 77051 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20725 77051 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10359736 99514 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283353 99514 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44394675 166372 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL427522 166372 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
38 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
722 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
CHEMBL42 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
DB00363 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
57391897 69309 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 69309 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
45270021 195164 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL550392 195164 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11382447 109666 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322519 109666 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
60149678 114517 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 114517 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
57267 1593 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
966 1593 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
CHEMBL8946 1593 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
DB15492 1593 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
9865858 163305 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
CHEMBL418854 163305 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
49798879 10611 6 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1170096 10611 6 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44319369 205819 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 205819 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
44380716 59087 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL169631 59087 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44324980 207421 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
CHEMBL94015 207421 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
10310103 107312 0 None -1778 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 107312 0 None -1778 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
9865920 107533 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL318739 107533 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
9887092 102674 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL304584 102674 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
71658338 90410 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386623 90410 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10569690 207073 11 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
CHEMBL91821 207073 11 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
73346042 91834 5 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91834 5 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
135398737 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
38 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
722 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
CHEMBL42 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
DB00363 958 93 None -13 89 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
56649648 67855 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 67855 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44426499 142065 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387951 142065 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
11451703 139018 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 139018 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
12050195 203284 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64696 203284 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
130431287 171217 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4459533 171217 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
44315403 205471 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 205471 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
44278456 99886 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28596 99886 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
122205438 137400 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 137400 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
11121216 30139 0 None -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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
128054 205141 10 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL7806 205141 10 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
127032085 139388 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 139388 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
10247720 13054 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 13054 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 13054 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
135398737 958 93 None -13 89 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
38 958 93 None -13 89 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
722 958 93 None -13 89 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
CHEMBL42 958 93 None -13 89 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
DB00363 958 93 None -13 89 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
49798853 14309 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1169895 14309 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199932 14309 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10254390 71688 0 None -5623 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
CHEMBL196476 71688 0 None -5623 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
10961938 119539 0 None -1202 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
CHEMBL345820 119539 0 None -1202 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
145993377 166968 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287471 166968 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
11071135 208008 0 None -3311 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 208008 0 None -3311 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
137646281 157806 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157806 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
44336003 5623 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
CHEMBL107755 5623 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
44336100 109776 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
CHEMBL323213 109776 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
30743524 4895 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104498 4895 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
44336031 5212 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106170 5212 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657946 90396 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386609 90396 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10559624 26389 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135932 26389 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10494689 11567 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180589 11567 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL134343 11567 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
10495881 109188 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL321513 109188 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
30616772 4788 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104063 4788 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
127028183 139316 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 139316 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
9886609 165329 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
CHEMBL423499 165329 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
127027238 139411 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 139411 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
44264641 204802 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7505 204802 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
12581219 25262 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
CHEMBL134866 25262 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
137645416 157927 0 None - 1 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4
ChEMBL 302 3 1 5 1.5 CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2n1C 10.6019/CHEMBL5212743
CHEMBL4084419 157927 0 None - 1 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4
ChEMBL 302 3 1 5 1.5 CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2n1C 10.6019/CHEMBL5212743
10567839 207033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
CHEMBL91585 207033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
44278853 105797 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL31269 105797 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
10567839 207033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91585 207033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
10636896 18884 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL128313 18884 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10688157 15581 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
CHEMBL122116 15581 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
10636896 18884 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL128313 18884 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
118719925 115779 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354072 115779 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
71658077 90403 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386616 90403 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
9884771 16598 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124050 16598 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
137657427 159559 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4102628 159559 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11570471 141917 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL386986 141917 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL4579981 214018 11 None - 1 Human 5.1 pKi = 5.1 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4
ChEMBL None None None Cc1ccc2[nH]c(CNCCCc3ccncc3)cc(=O)c2c1 10.6019/CHEMBL5210307
11092112 207628 0 None -13489 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 207628 0 None -13489 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
46231924 200578 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 200578 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
118719807 115734 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353910 115734 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44403220 71926 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL197214 71926 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
10375676 115203 37 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL334472 115203 37 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
56597938 3940 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 3940 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 3940 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
122189394 123249 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613880 123249 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
22727361 13257 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1191469 13257 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL542573 13257 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
155530763 171569 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 171569 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
137655594 158640 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4092462 158640 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
142590721 180274 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4750660 180274 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
44431474 87483 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL233404 87483 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
57393628 69313 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 69313 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
440229 87511 53 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 87511 53 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
10895106 32227 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL140968 32227 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
44335979 5104 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL105595 5104 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
127052458 140740 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140740 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
22727322 13938 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1196566 13938 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL557409 13938 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
154706030 176545 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 176545 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 176545 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
127052458 140740 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 140740 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
44340376 110646 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110646 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10895106 32227 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL140968 32227 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
72164182 92150 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 92150 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
25072946 111784 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
CHEMBL3287400 111784 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
44405530 141312 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL383383 141312 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
56837419 69304 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 69304 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
15888352 124113 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
CHEMBL36337 124113 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
90644066 112040 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289653 112040 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
5280343 188275 124 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL1520590 188275 124 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL50 188275 124 None 1 32 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
44591086 189581 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
CHEMBL514590 189581 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
44395709 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456429 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL556361 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395709 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456429 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL556361 174898 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44436302 90634 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238917 90634 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
44273896 99474 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283142 99474 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
9888211 21416 13 None -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO 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 -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11347425 205119 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77850 205119 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
12997412 9192 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL110349 9192 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
11168182 3534 25 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
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 -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
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 -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
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
57326584 74065 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022273 74065 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
44394618 66191 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184388 66191 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
44335918 5137 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105745 5137 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
233952 199699 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59324 199699 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
44335876 5056 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105304 5056 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44336314 109641 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL322326 109641 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
233952 199699 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59324 199699 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
11739255 80018 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 80018 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10425450 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
15840856 99829 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL285577 99829 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
44436596 91996 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241631 91996 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
10359736 99514 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
CHEMBL283353 99514 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
137655735 158992 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 158992 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
22100943 103135 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
CHEMBL307869 103135 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
119570 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
91864602 140738 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140738 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
10318141 207090 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
CHEMBL91938 207090 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
10318141 207090 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91938 207090 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1016/j.ejmech.2020.113034
12888943 9569 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL112395 9569 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
25131876 86192 0 None -12 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
CHEMBL2312227 86192 0 None -12 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
137640189 156953 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 156953 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
10737474 101353 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 101353 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
53363199 63852 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803051 63852 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
22100957 204266 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71208 204266 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10620139 206774 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
CHEMBL90173 206774 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
9945233 205092 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 205092 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
119570 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3159 96 None -10 40 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2812861 208441 6 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL99967 208441 6 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
10324985 76781 8 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 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 -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 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 -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
2389 3331 118 None -22 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -22 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -22 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -22 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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 -22 67 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 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
2 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
2 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
54562 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
CHEMBL240773 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
2 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3261 23 None -2 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44284013 139230 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL37885 139230 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10450880 207164 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL92373 207164 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10685891 11597 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180627 11597 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL135357 11597 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
3645619 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
10450880 207164 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL92373 207164 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
57401820 70161 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 70161 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401820 70161 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940409 70161 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
118709175 113423 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318848 113423 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
3645619 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
44323780 112575 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL330108 112575 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
9819770 141085 10 None 208 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/j.ejmech.2020.113141
CHEMBL38262 141085 10 None 208 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/j.ejmech.2020.113141
44323780 112575 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL330108 112575 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
44222483 196251 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 196251 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
9819770 141085 10 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38262 141085 10 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
137653577 158873 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
CHEMBL4095082 158873 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
44360992 119404 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
CHEMBL344677 119404 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
228 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
13091359 113539 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113539 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
681 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
940 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
947 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
CHEMBL59 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
DB00988 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
44360992 119404 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
CHEMBL344677 119404 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
CHEMBL5278957 194005 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 363 3 2 2 3.4 CC(C)N1C[C@H](C)[C@H](NC(=O)c2cc3ccc(Br)cc3[nH]2)C1 10.1016/j.ejmech.2020.113141
11776546 203236 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL64508 203236 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
11776546 203236 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
CHEMBL64508 203236 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
10392655 200265 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL59713 200265 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
10392655 200265 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
CHEMBL59713 200265 0 None -389 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
72205046 91947 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414357 91947 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
122177643 121211 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 121211 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
11452692 58912 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688991 58912 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
11452692 58912 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688991 58912 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
155512662 169655 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
CHEMBL4437341 169655 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
71456890 81827 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164351 81827 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44415689 139109 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 139109 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44336004 5433 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
CHEMBL107338 5433 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
242 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
242 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 470 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
72737767 114520 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 114520 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
134144304 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44283963 140187 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL38046 140187 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
2274 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
154705015 176514 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 176514 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 176514 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
71062829 160134 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
CHEMBL4108986 160134 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
44591043 176812 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL460855 176812 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
130431343 174516 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4555307 174516 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44454685 95053 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
CHEMBL255163 95053 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
134144304 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 154493 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
57391895 69301 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 69301 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
155513053 169698 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 169698 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11405107 199063 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
CHEMBL58662 199063 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
11808247 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11314005 109533 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL322175 109533 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
162645252 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
11808247 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 18075 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10961938 119539 0 None -1380 8 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
CHEMBL345820 119539 0 None -1380 8 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
71658207 90408 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386621 90408 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
4209 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
4893 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
503 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
5385 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
CHEMBL2 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
DB00457 3163 75 None -1318 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
127052486 140823 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 140823 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
46231926 200579 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 200579 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10689266 207044 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
CHEMBL91658 207044 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
10689266 207044 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1016/j.ejmech.2020.113034
CHEMBL91658 207044 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1016/j.ejmech.2020.113034
162645252 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 183625 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
56649649 67857 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 67857 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44431483 167645 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL430167 167645 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137655451 158853 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 158853 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
56833463 68336 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916552 68336 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
11783703 41034 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148752 41034 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11560697 10610 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1170095 10610 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
127052486 140823 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 140823 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
154705128 176291 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4454872 176291 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 176291 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL5079903 214651 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154724609 176599 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514800 176599 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 176599 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154726922 176541 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442936 176541 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597157 176541 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
118709171 113418 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318843 113418 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45483655 198115 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
CHEMBL574534 198115 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
11151135 109417 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322002 109417 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
154706123 176288 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 176288 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 176288 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
168286314 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5196213 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
127035062 136451 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 136451 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
91864602 140738 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 140738 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
168286314 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5196213 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
168286314 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 191659 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
56681925 66366 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1813589 66366 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1851628 66366 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
44338149 110337 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL323997 110337 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
44360984 35081 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
CHEMBL143352 35081 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
44316315 205519 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL80845 205519 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10623982 207052 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL91693 207052 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22100965 203760 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
CHEMBL67982 203760 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
44372154 54225 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160749 54225 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
44360984 35081 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
CHEMBL143352 35081 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
16007117 80036 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 80036 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
137660707 159299 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4099666 159299 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
118719795 115722 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353898 115722 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
154725749 176688 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4453478 176688 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598388 176688 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
11849229 138174 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 138174 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
22727347 13030 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189897 13030 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL539744 13030 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11775107 166216 0 None -26 3 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL426629 166216 0 None -26 3 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
863787 66291 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 66291 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
164610259 185107 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4856161 185107 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
49782841 17652 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
CHEMBL1258382 17652 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
137642033 158144 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4087217 158144 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
44438237 93659 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL246855 93659 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
127053222 139369 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 139369 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
57398352 70162 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940410 70162 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
90644228 111786 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 111786 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709177 113425 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318850 113425 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
135442113 118992 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL342536 118992 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
155533824 171898 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4469777 171898 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
51353676 60181 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1689002 60181 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1739784 60181 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
51353992 60211 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1689009 60211 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1739965 60211 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
9980998 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL139926 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL2112911 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
9980998 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 31035 0 None -1148 8 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
53248365 62086 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 62086 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
53326601 58911 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
CHEMBL1688990 58911 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
53326601 58911 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688990 58911 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
135398737 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
3645619 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
975 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
CHEMBL45244 3034 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
10950176 45012 1 None -33 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152391 45012 1 None -33 4 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
155530733 171579 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4465002 171579 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10158455 119970 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL349833 119970 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
10495652 36575 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL144835 36575 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
1613 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
205 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
3964 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
CHEMBL831 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
DB00408 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
163091 494 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
22 494 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
CHEMBL504548 494 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
10643780 119395 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL344602 119395 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
10594113 204910 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76090 204910 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
11131951 49921 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
CHEMBL156845 49921 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
15467369 100928 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL293956 100928 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
90644230 111790 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 111790 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
23364995 113420 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318845 113420 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11292776 5585 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107691 5585 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
44283757 137862 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37604 137862 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
57345617 70456 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946123 70456 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
127028505 139333 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 139333 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
76518514 113537 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 113537 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
122177645 121213 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 121213 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
10356955 12988 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1189601 12988 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL539057 12988 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
57398351 70158 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 70158 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57398351 70158 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940406 70158 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
11504230 78217 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 78217 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
71461481 84070 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207632 84070 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
76321556 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
2099556 205053 7 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL77151 205053 7 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
155566403 175936 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4587645 175936 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
76321556 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 106377 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
54585810 61604 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771108 61604 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
44403225 70548 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194755 70548 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
9129986 5058 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105317 5058 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44412268 78367 9 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL211026 78367 9 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
25142456 82406 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 82406 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
11849268 168797 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL437532 168797 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
118719797 115724 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353900 115724 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
71086428 151553 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3963122 151553 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
8704110 66601 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 66601 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
127698 116000 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
CHEMBL335545 116000 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
127698 116000 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
CHEMBL335545 116000 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
127046949 139909 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 139909 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
135398737 958 93 None -13 89 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
38 958 93 None -13 89 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
722 958 93 None -13 89 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
CHEMBL42 958 93 None -13 89 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
DB00363 958 93 None -13 89 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
11630058 141375 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
CHEMBL383805 141375 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
142590701 179521 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4741279 179521 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
132060720 162489 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 162489 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL5270824 193654 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 0 5 2.9 Fc1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5270824 193654 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 0 5 2.9 Fc1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
11699516 141634 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL385289 141634 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
8690650 4767 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103900 4767 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
154726381 176527 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 176527 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 176527 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44269820 45041 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
CHEMBL15242 45041 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
56649650 67858 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 67858 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
9882594 110383 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
CHEMBL324270 110383 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
9910451 164130 0 None -912 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 164130 0 None -912 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11152225 5127 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
CHEMBL105690 5127 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
127046948 140070 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 140070 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44582705 186996 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186996 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
9980998 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL139926 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL2112911 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
9928553 17440 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL125763 17440 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
53359025 62353 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 62353 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
9980998 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
9980998 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL139926 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL2112911 31035 0 None -1148 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
10522334 105412 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
CHEMBL311832 105412 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
44323870 111591 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL328246 111591 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
44393737 65761 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 65761 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
49798799 14358 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1172209 14358 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1200150 14358 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
20256387 4772 2 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103951 4772 2 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
122181326 121867 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL3590077 121867 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137636498 156196 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 156196 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
122181326 121867 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 121867 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
749986 204263 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL71173 204263 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
49798835 14361 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172213 14361 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200153 14361 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
15508240 110527 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL325104 110527 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
49798857 14315 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1170085 14315 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1199947 14315 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
154725276 176290 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4456964 176290 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 176290 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
23290944 81826 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 81826 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44336055 5350 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106897 5350 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
145993990 167354 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294577 167354 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
137651576 157488 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1016/j.ejmech.2020.113141
CHEMBL4079495 157488 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1016/j.ejmech.2020.113141
155563301 175250 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 175250 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168284020 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5190239 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168284020 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
137651576 157488 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
CHEMBL4079495 157488 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
164612933 185000 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4854512 185000 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
164627090 186558 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878121 186558 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
9843032 108533 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL320067 108533 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
168284020 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5190239 191253 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
44431468 88270 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234824 88270 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10110263 12992 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189648 12992 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539235 12992 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
15508242 165249 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL422959 165249 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
45270813 196689 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL564709 196689 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
154704418 176587 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4546749 176587 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 176587 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
12581203 25073 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134701 25073 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
25141538 56241 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 56241 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
681 1465 72 None -2 39 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1465 72 None -2 39 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1465 72 None -2 39 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1465 72 None -2 39 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1465 72 None -2 39 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
44330694 107588 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL318949 107588 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
44403224 71915 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
CHEMBL197195 71915 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
22100968 204104 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL70267 204104 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
11230330 135187 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 135187 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
44415593 80247 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 80247 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
154725234 176292 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4585289 176292 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 176292 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
11547151 84365 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221843 84365 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
44275807 98970 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98970 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
155515301 169967 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4441888 169967 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
49798874 14351 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1171630 14351 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1200106 14351 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
122189391 123246 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 123246 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
16090814 81581 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81581 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
142590731 183082 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4794406 183082 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
154704536 176447 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4467528 176447 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4596340 176447 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
11637457 73087 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 73087 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
51353678 60187 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1689004 60187 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1739810 60187 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
44380921 58329 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168274 58329 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
11212939 69160 0 None -10 3 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL192439 69160 0 None -10 3 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
44336035 5294 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106598 5294 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
135 2532 43 None - 58 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None - 58 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None - 58 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None - 58 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None - 58 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1911 93 None -3 83 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -3 83 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -3 83 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -3 83 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -3 83 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
9952220 98256 6 None -8 4 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
CHEMBL274491 98256 6 None -8 4 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
188942 2818 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
3297 2818 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
979 2818 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
CHEMBL103772 2818 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
2470 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
2470 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
3300 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
3300 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
5265 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
5265 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
99 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
99 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
CHEMBL267930 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
CHEMBL267930 3653 50 None -20 59 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
4452 2762 19 None -7 19 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
983 2762 19 None -7 19 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
CHEMBL20734 2762 19 None -7 19 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
4452 2762 19 3H-YM 09151-2 -7 19 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2762 19 3H-YM 09151-2 -7 19 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2762 19 3H-YM 09151-2 -7 19 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
2470 3653 50 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -4 59 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
16363 596 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 596 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 596 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 596 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 596 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2470 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -20 59 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 216278 0 UNDEFINED 4 12 Human 10.1 pKi = 10.1 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
2 3261 23 3H-SPIPERONE -2 29 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 23 3H-SPIPERONE -2 29 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 23 3H-SPIPERONE -2 29 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
2389 3331 118 3H-SPIPERONE -22 67 Human 9.6 pKi = 9.6 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 -22 67 Human 9.6 pKi = 9.6 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-SPIPERONE -22 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 UNDEFINED -22 67 Human 9.6 pKi = 9.6 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-SPIPERONE -22 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 UNDEFINED -22 67 Human 9.6 pKi = 9.6 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-SPIPERONE -22 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 UNDEFINED -22 67 Human 9.6 pKi = 9.6 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-SPIPERONE -22 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 UNDEFINED -22 67 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1911 93 3H-SPIPERONE -3 83 Human 9.5 pKi = 9.5 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-SPIPERONE -3 83 Human 9.5 pKi = 9.5 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-SPIPERONE -3 83 Human 9.5 pKi = 9.5 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-SPIPERONE -3 83 Human 9.5 pKi = 9.5 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-SPIPERONE -3 83 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5567 42802 27 UNDEFINED -11 8 Human 9.5 pKi = 9.5 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 UNDEFINED -11 8 Human 9.5 pKi = 9.5 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
2470 3653 50 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -4 59 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1238 203174 24 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
3303 2244 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 2244 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 2244 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
11976 920 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1353 1911 93 3H-SPIROPERIDOL -3 83 Human 9.1 pKi = 9.1 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-SPIROPERIDOL -3 83 Human 9.1 pKi = 9.1 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-SPIROPERIDOL -3 83 Human 9.1 pKi = 9.1 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-SPIROPERIDOL -3 83 Human 9.1 pKi = 9.1 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-SPIROPERIDOL -3 83 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 4143 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 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 -66 53 Human 9.1 pKi = 9.1 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 -66 53 Human 9.1 pKi = 9.1 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 -66 53 Human 9.1 pKi = 9.1 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 -66 53 Human 9.1 pKi = 9.1 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-Haloperidol -3 83 Human 9.1 pKi = 9.1 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-SPIPERONE -3 83 Human 9.1 pKi = 9.1 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 -3 83 Human 9.1 pKi = 9.1 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-Haloperidol -3 83 Human 9.1 pKi = 9.1 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-SPIPERONE -3 83 Human 9.1 pKi = 9.1 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 -3 83 Human 9.1 pKi = 9.1 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-Haloperidol -3 83 Human 9.1 pKi = 9.1 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-SPIPERONE -3 83 Human 9.1 pKi = 9.1 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 -3 83 Human 9.1 pKi = 9.1 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-Haloperidol -3 83 Human 9.1 pKi = 9.1 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-SPIPERONE -3 83 Human 9.1 pKi = 9.1 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 -3 83 Human 9.1 pKi = 9.1 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-Haloperidol -3 83 Human 9.1 pKi = 9.1 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-SPIPERONE -3 83 Human 9.1 pKi = 9.1 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 -3 83 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3168 9262 92 UNDEFINED -4 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9262 92 UNDEFINED -4 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
2435 3590 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 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-SPIPERONE -10 48 Human 9.1 pKi = 9.1 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-SPIPERONE -10 48 Human 9.1 pKi = 9.1 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-SPIPERONE -10 48 Human 9.1 pKi = 9.1 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-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3590 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 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-Sertindole -10 48 Human 9.0 pKi = 9 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-Sertindole -10 48 Human 9.0 pKi = 9 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-Sertindole -10 48 Human 9.0 pKi = 9 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-Sertindole -10 48 Human 9.0 pKi = 9 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-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2726 919 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2470 3653 50 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -20 59 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 3805 58 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3805 58 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SPIPERONE -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 UNDEFINED -8 55 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 958 93 3H-Clozapine -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-SPIPERONE -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 UNDEFINED -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Clozapine -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SPIPERONE -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Clozapine -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SPIPERONE -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Clozapine -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SPIPERONE -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Clozapine -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SPIPERONE -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -13 89 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 UNDEFINED -14 17 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2914 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3303 2244 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 2244 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 2244 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
16362 3125 71 R-SAT -20 30 Human 8.7 pKi = 8.7 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 R-SAT -20 30 Human 8.7 pKi = 8.7 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 R-SAT -20 30 Human 8.7 pKi = 8.7 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 R-SAT -20 30 Human 8.7 pKi = 8.7 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 R-SAT -20 30 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 107531 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1613 2348 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 3805 58 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SPIPERONE -3 55 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
115368 3056 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2112 3056 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
7556 3056 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
CHEMBL1472975 3056 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
DB08922 3056 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2435 3590 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 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-SPIPERONE -19 48 Rat 8.0 pKi = 8 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-SPIPERONE -19 48 Rat 8.0 pKi = 8 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-SPIPERONE -19 48 Rat 8.0 pKi = 8 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-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1353 1911 93 3H-SPIPERONE -4 83 Rat 8.0 pKi = 8.0 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-SPIPERONE -4 83 Rat 8.0 pKi = 8.0 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-SPIPERONE -4 83 Rat 8.0 pKi = 8.0 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-SPIPERONE -4 83 Rat 8.0 pKi = 8.0 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-SPIPERONE -4 83 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
100 3805 58 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SPIPERONE -8 55 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
4257 78255 30 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
CHEMBL2106650 78255 30 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
25139335 184318 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
CHEMBL484203 184318 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
242 470 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5281878 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 R-SAT -14 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 4143 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
15387 45822 55 R-SAT -35 24 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 R-SAT -35 24 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
54477 84653 36 R-SAT -14 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 R-SAT -14 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
164512405 215949 0 3H-SPIPERONE -10 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
119192 2481 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1582 2481 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
CHEMBL506981 2481 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
DB06455 2481 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
134 2514 24 3H-NMSP -8511 67 Human 5.0 pKi = 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-NMSP -8511 67 Human 5.0 pKi = 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-NMSP -8511 67 Human 5.0 pKi = 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-NMSP -8511 67 Human 5.0 pKi = 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-NMSP -8511 67 Human 5.0 pKi = 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
15897 2862 0 3H-NMSP -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-NMSP -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-NMSP -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
128563 3464 33 3H-NMSP -2398 42 Rat 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-NMSP -2398 42 Rat 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-NMSP -2398 42 Rat 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-NMSP -2398 42 Rat 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
189 3492 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 3492 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 3492 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
185 4006 60 3H-NMSP -7244 37 Human 5.0 pKi = 5 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-NMSP -7244 37 Human 5.0 pKi = 5 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-NMSP -7244 37 Human 5.0 pKi = 5 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-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2662 11384 131 3H-NMSP -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-NMSP -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
10297 27112 30 3H-NMSP -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-NMSP -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
156391 46800 99 3H-NMSP -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-NMSP -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-NMSP -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
10624 70300 19 3H-NMSP -776 33 Human 5.0 pKi = 5 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-NMSP -776 33 Human 5.0 pKi = 5 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-NMSP -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 94233 100 3H-NMSP -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-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
24840389 115213 4 3H-SPIPERONE -7413 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 115213 4 3H-SPIPERONE -7413 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
446220 133521 14 3H-NMSP -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-NMSP -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-NMSP -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1615 167791 24 3H-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 24 3H-NMSP -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-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
3672 192533 136 3H-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-NMSP -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-Methylspiperone -275 33 Rat 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-Methylspiperone -275 33 Rat 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
3821 204718 17 3H-N-Methylspiperone -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-N-Methylspiperone -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4054 205501 72 3H-NMSP -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-NMSP -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-NMSP -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
3337 206367 27 3H-NMSP -1513 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-NMSP -1513 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-NMSP -1513 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-NMSP -1513 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-NMSP -1513 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
164512405 215949 0 3H-SPIPERONE -33 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
11954224 215953 0 3H-NMSP -141253 58 Human 5.0 pKi = 5 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
None 215993 0 3H-N-Methylspiperone -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
25137849 216179 0 3H-NMSP -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-NMSP -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 216239 0 3H-NMSP -95499 30 Rat 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-NMSP -1 33 Rat 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-NMSP -1 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 0 3H-NMSP -1 33 Rat 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-NMSP -1 33 Rat 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-NMSP -1 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 0 3H-NMSP -1 39 Rat 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-NMSP -1 38 Rat 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-NMSP -1 30 Rat 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-NMSP -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-NMSP -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-Methylspiperone -16 28 Rat 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
None 216329 0 3H-Methylspiperone -3 28 Rat 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-Methylspiperone -281 28 Rat 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-Methylspiperone -1 28 Rat 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-NMSP -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-NMSP -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-NMSP -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-NMSP -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
119828 216394 0 3H-NMSP -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 216450 0 3H-SPIPERONE -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216450 0 UNDEFINED -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216489 0 3H-NMSP -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
164512405 215949 0 3H-SPIPERONE -10 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
135409468 2035 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
44395711 174899 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL456430 174899 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL537183 174899 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
1353 1911 93 UNDEFINED -3 83 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 UNDEFINED -3 83 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 UNDEFINED -3 83 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 UNDEFINED -3 83 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 UNDEFINED -3 83 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 4143 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 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-NMSP -66 53 Human 7.0 pKi = 7.0 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-NMSP -66 53 Human 7.0 pKi = 7.0 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-NMSP -66 53 Human 7.0 pKi = 7.0 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-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3256 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
9906978 42711 2 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42711 2 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
25139329 187103 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL491466 187103 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
2274 3173 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 3256 77 3H-SPIPERONE -173 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-SPIPERONE -173 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-SPIPERONE -173 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-SPIPERONE -173 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-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
37459 746 13 3H-SPIPERONE -123 25 Human 6.9 pKi = 6.9 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-SPIPERONE -123 25 Human 6.9 pKi = 6.9 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-SPIPERONE -123 25 Human 6.9 pKi = 6.9 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
1613 2348 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2348 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 3805 58 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SPIPERONE -3 55 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2726 919 68 3H-SPIPERONE -10 72 Rat 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-SPIPERONE -10 72 Rat 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-SPIPERONE -10 72 Rat 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-SPIPERONE -10 72 Rat 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-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1353 1911 93 UNDEFINED -3 83 Human 7.9 pKi = 7.9 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 -3 83 Human 7.9 pKi = 7.9 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 -3 83 Human 7.9 pKi = 7.9 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 -3 83 Human 7.9 pKi = 7.9 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 -3 83 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
277 1301 62 3H-Methylspiperone -144 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 3H-Methylspiperone -144 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 3H-Methylspiperone -144 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 3H-Methylspiperone -144 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 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
None 216229 0 3H-YM 09151-2 15 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
2337 3256 77 3H-NMSP -114 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 3H-NMSP -114 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 3H-NMSP -114 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 3H-NMSP -114 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 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44591089 189482 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
CHEMBL513776 189482 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
2 3261 23 3H-SPIPERONE -2 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 23 3H-SPIPERONE -2 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 23 3H-SPIPERONE -2 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
4978 216328 0 3H-Methylspiperone -2 28 Rat 5.9 pKi = 5.9 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
119570 3159 96 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-SPIPERONE -10 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
6603820 95774 19 3H-SCH23390 -1 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95774 19 3H-SCH23390 -1 13 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
None 216229 0 3H-SPIPERONE 15 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
1712 2492 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
101 3822 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3822 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3822 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
279 1661 26 3H-SPIPERONE -26 18 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 26 3H-SPIPERONE -26 18 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 26 3H-SPIPERONE -26 18 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
5281878 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 R-SAT -14 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 216160 0 3H-YM 09151-2 -1 4 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 233 4 1 2 3.1 CCCNC1CCC2=C(C1C)C=CC=C2OC None
3033769 3281 61 3H-YM 09151-2 -562 19 Human 5.9 pKi = 5.9 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-YM 09151-2 -562 19 Human 5.9 pKi = 5.9 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-YM 09151-2 -562 19 Human 5.9 pKi = 5.9 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-YM 09151-2 -562 19 Human 5.9 pKi = 5.9 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-YM 09151-2 -562 19 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
15387 45822 55 3H-YM 09151-2 -35 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-YM 09151-2 -35 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
135398745 2914 112 3H-SPIPERONE -10 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-SPIPERONE -10 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-SPIPERONE -10 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-SPIPERONE -10 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
5467 205928 43 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 205928 43 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
2274 3173 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
25139332 184319 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL484204 184319 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
None 217357 0 UNDEFINED -380 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 451 3 0 7 3.9 CC1=NC2=C(C=C1)C3=C(C=C2)OCC(O3)CN4CCN(CC4)C5=NC6=C(C=C5)C=C(C=C6)C#N None
3663 99967 83 3H-Methylspiperone -42 29 Rat 5.8 pKi = 5.8 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-Methylspiperone -42 29 Rat 5.8 pKi = 5.8 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
1353 1911 93 3H-NMSP -3 83 Human 7.8 pKi = 7.8 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-NMSP -3 83 Human 7.8 pKi = 7.8 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-NMSP -3 83 Human 7.8 pKi = 7.8 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-NMSP -3 83 Human 7.8 pKi = 7.8 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-NMSP -3 83 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2914 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2726 919 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
133633 2241 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
177 2241 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
CHEMBL445102 2241 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
2435 3590 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 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-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 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-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 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-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 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-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
104911 216019 0 3H-NMSP -67 37 Human 7.8 pKi = 7.8 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
2389 3331 118 3H-SPIPERONE -30 67 Rat 7.8 pKi = 7.8 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-SPIPERONE -30 67 Rat 7.8 pKi = 7.8 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-SPIPERONE -30 67 Rat 7.8 pKi = 7.8 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-SPIPERONE -30 67 Rat 7.8 pKi = 7.8 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-SPIPERONE -30 67 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2337 3256 77 3H-NEMONAPRIDE -114 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-NEMONAPRIDE -114 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-NEMONAPRIDE -114 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-NEMONAPRIDE -114 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-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
6852400 215937 0 R-SAT -794 22 Human 6.8 pKi = 6.8 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 R-SAT -794 22 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
209 3057 97 UNDEFINED -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 UNDEFINED -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 UNDEFINED -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 UNDEFINED -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 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
100 3805 58 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-NMSP -8 55 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44395741 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44395741 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 181581 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44350664 118149 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL340816 118149 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553417 118149 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
2389 3331 118 3H-NEMONAPRIDE -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3331 118 R-SAT -22 67 Human 7.7 pKi = 7.7 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-NEMONAPRIDE -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 R-SAT -22 67 Human 7.7 pKi = 7.7 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-NEMONAPRIDE -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 R-SAT -22 67 Human 7.7 pKi = 7.7 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-NEMONAPRIDE -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 R-SAT -22 67 Human 7.7 pKi = 7.7 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-NEMONAPRIDE -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 R-SAT -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
103 4153 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2389 3331 118 3H-NMSP -22 67 Human 7.7 pKi = 7.7 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-NMSP -22 67 Human 7.7 pKi = 7.7 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-NMSP -22 67 Human 7.7 pKi = 7.7 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-NMSP -22 67 Human 7.7 pKi = 7.7 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-NMSP -22 67 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
44591045 176737 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
CHEMBL460223 176737 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
25139478 184956 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL485384 184956 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
135398745 2914 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
214 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 216342 0 3H-SPIPERONE -3 19 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
13091273 182438 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL478617 182438 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553327 182438 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
25139479 184317 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
CHEMBL484202 184317 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
191 403 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1353 1911 93 3H-SPIPERONE -3 83 Human 8.7 pKi = 8.7 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-SPIPERONE -3 83 Human 8.7 pKi = 8.7 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-SPIPERONE -3 83 Human 8.7 pKi = 8.7 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-SPIPERONE -3 83 Human 8.7 pKi = 8.7 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-SPIPERONE -3 83 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2914 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4249 78179 34 UNDEFINED -7 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 78179 34 UNDEFINED -7 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
1353 1911 93 3H-SPIPERONE -4 83 Rat 8.6 pKi = 8.6 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-SPIPERONE -4 83 Rat 8.6 pKi = 8.6 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-SPIPERONE -4 83 Rat 8.6 pKi = 8.6 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-SPIPERONE -4 83 Rat 8.6 pKi = 8.6 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-SPIPERONE -4 83 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 2006 111 UNDEFINED -11 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 UNDEFINED -11 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 UNDEFINED -11 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 UNDEFINED -11 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 UNDEFINED -11 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1353 1911 93 3H-NEMONAPRIDE -3 83 Human 8.5 pKi = 8.5 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-YM 09151-2 -3 83 Human 8.5 pKi = 8.5 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-NEMONAPRIDE -3 83 Human 8.5 pKi = 8.5 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-YM 09151-2 -3 83 Human 8.5 pKi = 8.5 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-NEMONAPRIDE -3 83 Human 8.5 pKi = 8.5 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-YM 09151-2 -3 83 Human 8.5 pKi = 8.5 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-NEMONAPRIDE -3 83 Human 8.5 pKi = 8.5 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-YM 09151-2 -3 83 Human 8.5 pKi = 8.5 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-NEMONAPRIDE -3 83 Human 8.5 pKi = 8.5 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-YM 09151-2 -3 83 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2726 919 68 3H-SCH23390 -10 72 Rat 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-SCH23390 -10 72 Rat 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-SCH23390 -10 72 Rat 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-SCH23390 -10 72 Rat 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-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135409468 2035 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
164512405 215949 0 3H-SPIPERONE -10 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
None 216013 0 3H-SPIPERONE -7 3 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 310 3 0 2 4.8 CN(C)CCC=C1C2=CC=CC=C2C=NC3=C1C=C(C=C3)Cl None
164512405 215949 0 UNDEFINED -10 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
2337 3256 77 3H-SPIPERONE -114 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-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-SPIPERONE -114 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-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-SPIPERONE -114 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-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-SPIPERONE -114 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-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-SPIPERONE -114 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-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
164512405 215949 0 3H-NEMONAPRIDE -10 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
11954259 215979 0 3H-NMSP -676 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
135398737 958 93 3H-SPIPERONE -13 89 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-SPIROPERIDOL -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIROPERIDOL -13 89 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 1661 26 UNDEFINED -4 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 26 UNDEFINED -4 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 26 UNDEFINED -4 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
164512405 215949 0 3H-SPIPERONE -10 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
21830793 91835 10 3H-8-OH-DPAT -144 45 Hybrid cattle 7.7 pKi = 7.7 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 -144 45 Hybrid cattle 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
44578445 181579 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
CHEMBL476933 181579 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
135398737 958 93 3H-SPIPERONE -13 89 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-SPIPERONE -7 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-SPIPERONE -13 89 Human 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-SPIPERONE -7 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-SPIPERONE -13 89 Human 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-SPIPERONE -7 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-SPIPERONE -13 89 Human 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-SPIPERONE -7 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-SPIPERONE -13 89 Human 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-SPIPERONE -7 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1353 1911 93 R-SAT -3 83 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 R-SAT -3 83 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 R-SAT -3 83 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 R-SAT -3 83 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 R-SAT -3 83 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44134711 215991 0 3H-SPIPERONE -275 14 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
100 3805 58 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-YM 09151-2 -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2337 3256 77 UNDEFINED -114 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 UNDEFINED -114 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 UNDEFINED -114 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 UNDEFINED -114 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 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
54477 84653 36 3H-NEMONAPRIDE -14 23 Human 5.7 pKi = 5.7 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-NEMONAPRIDE -14 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2337 3256 77 3H-N-Methylspiperone -114 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-N-Methylspiperone -114 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-N-Methylspiperone -114 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-N-Methylspiperone -114 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-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 216620 0 UNDEFINED -102 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
2726 919 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1662 50 3H-NEMONAPRIDE -77 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-NEMONAPRIDE -77 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-NEMONAPRIDE -77 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-NEMONAPRIDE -77 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-NEMONAPRIDE -77 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
65750 216446 0 R-SAT -1 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
15387 45822 55 3H-SPIPERONE -33 24 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-SPIPERONE -33 24 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
243 3202 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
179 400 115 3H-NMSP -50 49 Human 5.6 pKi = 5.6 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-NMSP -50 49 Human 5.6 pKi = 5.6 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-NMSP -50 49 Human 5.6 pKi = 5.6 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-NMSP -50 49 Human 5.6 pKi = 5.6 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-NMSP -50 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
3033769 3281 61 3H-SPIPERONE -288 19 Rat 6.6 pKi = 6.6 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-SPIPERONE -288 19 Rat 6.6 pKi = 6.6 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-SPIPERONE -288 19 Rat 6.6 pKi = 6.6 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-SPIPERONE -288 19 Rat 6.6 pKi = 6.6 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-SPIPERONE -288 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
2726 919 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1830 2590 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2590 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3033769 3281 61 3H-SPIPERONE -562 19 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3281 61 3H-SPIPERONE -288 19 Rat 5.6 pKi = 5.6 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-SPIPERONE -562 19 Human 5.6 pKi = 5.6 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-SPIPERONE -288 19 Rat 5.6 pKi = 5.6 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-SPIPERONE -562 19 Human 5.6 pKi = 5.6 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-SPIPERONE -288 19 Rat 5.6 pKi = 5.6 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-SPIPERONE -562 19 Human 5.6 pKi = 5.6 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-SPIPERONE -288 19 Rat 5.6 pKi = 5.6 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-SPIPERONE -562 19 Human 5.6 pKi = 5.6 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-SPIPERONE -288 19 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
54477 84653 36 3H-SPIPERONE -14 23 Human 5.6 pKi = 5.6 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-SPIPERONE -14 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
9906978 42711 2 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42711 2 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
3294 2006 111 3H-SPIPERONE -11 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-SPIPERONE -11 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-SPIPERONE -11 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-SPIPERONE -11 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-SPIPERONE -11 45 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
100 3805 58 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-NEMONAPRIDE -8 55 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 470 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 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-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 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-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 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-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 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-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
135398745 2914 112 3H-SPIPERONE -10 65 Human 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-SPIPERONE -10 65 Human 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-SPIPERONE -10 65 Human 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-SPIPERONE -10 65 Human 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
4249 78179 34 R-SAT -7 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 78179 34 R-SAT -7 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
44134711 215991 0 3H-SPIPERONE -275 14 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
44591042 176811 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
CHEMBL460854 176811 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
2435 3590 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
135398737 958 93 3H-YM 09151-2 -13 89 Human 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-YM 09151-2 -13 89 Human 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-YM 09151-2 -13 89 Human 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-YM 09151-2 -13 89 Human 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-YM 09151-2 -13 89 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
163839 2955 0 3H-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 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-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 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-Methylspiperone -15 7 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
54477 84653 36 3H-SPIPERONE -14 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84653 36 UNDEFINED -14 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84653 36 3H-SPIPERONE -38 23 Rat 5.6 pKi = 5.6 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-SPIPERONE -14 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 UNDEFINED -14 23 Human 5.6 pKi = 5.6 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-SPIPERONE -38 23 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
31101 729 40 3H-SPIPERONE -186 36 Human 6.6 pKi = 6.6 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-SPIPERONE -186 36 Human 6.6 pKi = 6.6 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-SPIPERONE -186 36 Human 6.6 pKi = 6.6 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-SPIPERONE -186 36 Human 6.6 pKi = 6.6 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-SPIPERONE -186 36 Human 6.6 pKi = 6.6 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
135398737 958 93 3H-Methylspiperone -7 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-Methylspiperone -7 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-Methylspiperone -7 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-Methylspiperone -7 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-Methylspiperone -7 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2348 53 3H-YM 09151-2 -2 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-YM 09151-2 -2 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-YM 09151-2 -2 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-YM 09151-2 -2 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-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
119570 3159 96 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-NMSP -10 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
135398745 2914 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3033769 3281 61 3H-SPIPERONE -562 19 Human 5.5 pKi = 5.5 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-SPIPERONE -562 19 Human 5.5 pKi = 5.5 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-SPIPERONE -562 19 Human 5.5 pKi = 5.5 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-SPIPERONE -562 19 Human 5.5 pKi = 5.5 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-SPIPERONE -562 19 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1353 1911 93 3H-SPIPERONE -3 83 Human 8.5 pKi = 8.5 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-SPIPERONE -3 83 Human 8.5 pKi = 8.5 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-SPIPERONE -3 83 Human 8.5 pKi = 8.5 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-SPIPERONE -3 83 Human 8.5 pKi = 8.5 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-SPIPERONE -3 83 Human 8.5 pKi = 8.5 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 -3 83 Human 8.5 pKi = 8.5 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 -3 83 Human 8.5 pKi = 8.5 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 -3 83 Human 8.5 pKi = 8.5 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 -3 83 Human 8.5 pKi = 8.5 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 -3 83 Human 8.5 pKi = 8.5 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-N-Methylspiperone -3 83 Human 8.5 pKi = 8.5 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-N-Methylspiperone -3 83 Human 8.5 pKi = 8.5 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-N-Methylspiperone -3 83 Human 8.5 pKi = 8.5 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-N-Methylspiperone -3 83 Human 8.5 pKi = 8.5 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-N-Methylspiperone -3 83 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 216230 0 3H-YM 09151-2 -3 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 359 1 2 2 3.7 CC(C)(C)C(=O)NC1CC2C(CC3=C(NC4=CC=CC2=C34)Cl)N(C1)C None
3691783 4764 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
CHEMBL103871 4764 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
CHEMBL146246 38278 0 3H-SPIPERONE -1 10 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 None
9906978 42711 2 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 42711 2 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
2470 3653 50 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 R-SAT -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 3805 58 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-SPIPERONE -3 55 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 958 93 3H-SPIROPERIDOL -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIROPERIDOL -13 89 Human 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-SPIROPERIDOL -13 89 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1662 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2914 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
16362 3125 71 3H-SPIPERONE -186 30 Rat 7.5 pKi = 7.5 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-SPIPERONE -186 30 Rat 7.5 pKi = 7.5 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-SPIPERONE -186 30 Rat 7.5 pKi = 7.5 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-SPIPERONE -186 30 Rat 7.5 pKi = 7.5 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-SPIPERONE -186 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
5074 3332 80 UNDEFINED -52 30 Human 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 UNDEFINED -52 30 Human 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 UNDEFINED -52 30 Human 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 UNDEFINED -52 30 Human 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
16106 118146 34 3H-SPIPERONE -1 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
16106 118146 34 UNDEFINED -1 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 3H-SPIPERONE -1 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 UNDEFINED -1 12 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
None 216415 0 3H-SPIPERONE -100 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
2337 3256 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 217163 0 UNDEFINED -120 3 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 366 3 2 2 4.8 C1CC2CC(CC1N2CC3=CNC4=CC=CC=C43)(C5=CC=C(C=C5)Cl)O None
2202 3132 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3132 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3132 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3132 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3132 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
135398745 2914 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
33630 178957 99 3H-SPIPERONE -5 28 Rat 7.5 pKi = 7.5 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-SPIPERONE -5 28 Rat 7.5 pKi = 7.5 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
25139180 184341 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL484357 184341 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
135398737 958 93 3H-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 3057 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2865 4143 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 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 -66 53 Human 7.5 pKi = 7.5 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 -66 53 Human 7.5 pKi = 7.5 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 -66 53 Human 7.5 pKi = 7.5 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 -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
214 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 4143 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 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-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 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-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 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-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 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-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
5567 42802 27 R-SAT -11 8 Human 6.5 pKi = 6.5 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 R-SAT -11 8 Human 6.5 pKi = 6.5 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
2 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
104870 98880 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98880 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98880 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
2 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 23 3H-SPIPERONE -2 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
135398737 958 93 3H-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 729 40 3H-SPIPERONE -489 36 Rat 6.5 pKi = 6.5 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-SPIPERONE -489 36 Rat 6.5 pKi = 6.5 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-SPIPERONE -489 36 Rat 6.5 pKi = 6.5 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-SPIPERONE -489 36 Rat 6.5 pKi = 6.5 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-SPIPERONE -489 36 Rat 6.5 pKi = 6.5 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
1830 2590 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3036864 202754 19 3H-SPIPERONE -14791 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202754 19 3H-SPIPERONE -14791 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202754 19 3H-SPIPERONE -14791 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202754 19 3H-SPIPERONE -14791 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1212 1662 50 3H-NMSP -77 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-NMSP -77 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-NMSP -77 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-NMSP -77 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-NMSP -77 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
54477 84653 36 3H-SPIPERONE -14 23 Human 5.4 pKi = 5.4 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-SPIPERONE -14 23 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2726 919 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
31101 729 40 3H-SPIPERONE -186 36 Human 6.4 pKi = 6.4 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-SPIPERONE -186 36 Human 6.4 pKi = 6.4 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-SPIPERONE -186 36 Human 6.4 pKi = 6.4 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-SPIPERONE -186 36 Human 6.4 pKi = 6.4 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-SPIPERONE -186 36 Human 6.4 pKi = 6.4 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
6917970 3691 61 3H-NMSP -851 34 Human 5.4 pKi = 5.4 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-NMSP -851 34 Human 5.4 pKi = 5.4 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-NMSP -851 34 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
37459 746 13 3H-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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 3H-NMSP -13 89 Human 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-NMSP -13 89 Human 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-NMSP -13 89 Human 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-NMSP -13 89 Human 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-NMSP -13 89 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 216415 0 3H-SPIPERONE -100 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
None 216232 0 3H-SPIPERONE 1 4 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 226 0 2 2 1.4 C1CCC(=O)NCCCCCC(=O)NCC1 None
186 1807 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1807 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1807 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
30137 2877 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2877 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2877 0 3H-SPIPERONE -10 10 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2470 3653 50 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-SPIPERONE -20 59 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25139181 184342 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
CHEMBL484358 184342 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
25058166 215960 0 3H-SPIPERONE -8 27 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 0 3H-SPIPERONE -8 27 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 3331 118 3H-SPIPERONE -22 67 Human 8.4 pKi = 8.4 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-SPIPERONE -22 67 Human 8.4 pKi = 8.4 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-SPIPERONE -22 67 Human 8.4 pKi = 8.4 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-SPIPERONE -22 67 Human 8.4 pKi = 8.4 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-SPIPERONE -22 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
37459 746 13 UNDEFINED -123 25 Human 8.4 pKi = 8.4 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 UNDEFINED -123 25 Human 8.4 pKi = 8.4 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 UNDEFINED -123 25 Human 8.4 pKi = 8.4 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
71240 207717 14 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
CHEMBL95636 207717 14 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
1588 2325 27 3H-SPIPERONE -16 44 Human 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-SPIPERONE -16 44 Human 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-SPIPERONE -16 44 Human 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-SPIPERONE -16 44 Human 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-SPIPERONE -16 44 Human 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
1613 2348 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
191 403 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
37459 746 13 3H-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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-SPIPERONE -123 25 Human 7.4 pKi = 7.4 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 3H-NEMONAPRIDE -13 89 Human 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-NEMONAPRIDE -13 89 Human 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-NEMONAPRIDE -13 89 Human 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-NEMONAPRIDE -13 89 Human 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-NEMONAPRIDE -13 89 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398737 958 93 3H-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 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-SPIPERONE -13 89 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11545813 181194 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
CHEMBL476109 181194 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
15387 45822 55 3H-SPIPERONE -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
15387 45822 55 UNDEFINED -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-SPIPERONE -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 UNDEFINED -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
3033769 3281 61 3H-NEMONAPRIDE -562 19 Human 5.4 pKi = 5.4 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-NEMONAPRIDE -562 19 Human 5.4 pKi = 5.4 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-NEMONAPRIDE -562 19 Human 5.4 pKi = 5.4 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-NEMONAPRIDE -562 19 Human 5.4 pKi = 5.4 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-NEMONAPRIDE -562 19 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
25058166 215960 0 3H-SPIPERONE -8 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 0 3H-SPIPERONE -8 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 216619 0 UNDEFINED -69 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
16362 3125 71 3H-SPIPERONE -186 30 Rat 7.4 pKi = 7.4 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-SPIPERONE -186 30 Rat 7.4 pKi = 7.4 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-SPIPERONE -186 30 Rat 7.4 pKi = 7.4 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-SPIPERONE -186 30 Rat 7.4 pKi = 7.4 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-SPIPERONE -186 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
1830 2590 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
214 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
214 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
25058166 215960 0 3H-YM 09151-2 -8 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 0 3H-YM 09151-2 -8 27 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1257 216378 0 3H-SPIPERONE 1 2 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCCC2C1CC3=C(C2)NN=C3 None
209 3057 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2448 99323 70 R-SAT -13 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99323 70 R-SAT -13 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
None 216619 0 UNDEFINED -69 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
1353 1911 93 3H-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4209 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3163 75 None -1318 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1353 1911 93 3H-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -4 83 Rat 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -4 83 Rat 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -4 83 Rat 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -4 83 Rat 8.3 pKi = 8.3 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-SPIPERONE -3 83 Human 8.3 pKi = 8.3 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-SPIPERONE -4 83 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5280343 188275 124 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188275 124 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188275 124 None 1 32 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 4779 101 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 101 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
2601 3780 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
176 398 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4189 206922 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206922 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206922 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
13091268 78224 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL210578 78224 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2274 3173 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1016 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3747 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
54477 84653 36 None -14 23 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 None -14 23 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
3198 205513 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205513 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205513 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1499 2091 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2091 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2091 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2091 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2091 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
7077 66959 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 66959 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL3925724 66959 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
1830 2590 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2590 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2247 505 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1577 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3703 110 None -10 21 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2337 3256 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
103 4153 61 3H-SPIPERONE -4 53 Rat 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-SPIPERONE -4 53 Rat 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-SPIPERONE -4 53 Rat 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-SPIPERONE -4 53 Rat 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-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
219050 3373 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3373 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3373 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
3117 207841 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207841 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
1212 1662 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1662 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2914 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 216620 0 UNDEFINED -102 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
37459 746 13 3H-SPIPERONE -123 25 Human 7.3 pKi = 7.3 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-SPIPERONE -123 25 Human 7.3 pKi = 7.3 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-SPIPERONE -123 25 Human 7.3 pKi = 7.3 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
242 470 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 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-NMSP -87 51 Rat 6.3 pKi = 6.3 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-NMSP -87 51 Rat 6.3 pKi = 6.3 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-NMSP -87 51 Rat 6.3 pKi = 6.3 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-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
44591088 189582 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL514591 189582 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
242 470 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 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-NMSP -104 51 Human 6.3 pKi = 6.3 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-NMSP -104 51 Human 6.3 pKi = 6.3 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-NMSP -104 51 Human 6.3 pKi = 6.3 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-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
164512405 215949 0 3H-SPIPERONE -33 13 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
44578446 181580 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
CHEMBL476934 181580 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
9429 202133 58 3H-SPIPERONE -251 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 None
CHEMBL609109 202133 58 3H-SPIPERONE -251 5 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 None
135398737 958 93 3H-N-Methylspiperone -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-N-Methylspiperone -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-N-Methylspiperone -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-N-Methylspiperone -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-N-Methylspiperone -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5311189 204841 11 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204841 11 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
135398737 958 93 UNDEFINED -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1577 3703 110 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 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 R-SAT -10 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
115237 55585 119 3H-NMSP -83 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-NMSP -83 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398737 958 93 3H-SPIPERONE -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SPIPERONE -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SPIPERONE -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SPIPERONE -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SPIPERONE -13 89 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
185 4006 60 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 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-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 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-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 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-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
202478 204687 20 3H-YM 09151-2 -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 20 3H-YM 09151-2 -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
1621 2429 17 3H-NMSP -181 45 Rat 7.3 pKi = 7.3 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-NMSP -181 45 Rat 7.3 pKi = 7.3 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-NMSP -181 45 Rat 7.3 pKi = 7.3 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-NMSP -181 45 Rat 7.3 pKi = 7.3 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-NMSP -181 45 Rat 7.3 pKi = 7.3 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
22065962 176796 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
CHEMBL460644 176796 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
None 216341 0 3H-SPIPERONE -74 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
10060538 4576 7 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 4576 7 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
2105 3054 37 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 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 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 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 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 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 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 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 3H-SPIPERONE -48 33 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
44591087 175750 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL458342 175750 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
33630 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor 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
2402 3370 62 None -2 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 None -2 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 None -2 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 None -2 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 None -2 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
681 1465 72 UNDEFINED -2 39 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 UNDEFINED -2 39 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 UNDEFINED -2 39 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 UNDEFINED -2 39 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 UNDEFINED -2 39 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
3191 102858 97 None -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
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 -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
15387 45822 55 None -35 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 None -35 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
31101 729 40 None -186 36 Human 8.2 pKi = 8.2 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 -186 36 Human 8.2 pKi = 8.2 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 -186 36 Human 8.2 pKi = 8.2 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 -186 36 Human 8.2 pKi = 8.2 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 -186 36 Human 8.2 pKi = 8.2 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
212 3806 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3806 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3806 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3806 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3806 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
104870 98880 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98880 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98880 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
1153 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1628 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2202 3132 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3132 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3132 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3132 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3132 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
10065083 32103 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
CHEMBL140872 32103 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
46 2905 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
71351 2905 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
CHEMBL2104619 2905 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
DB06229 2905 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
11653679 181191 1 UNDEFINED 3 11 Human 8.2 pKi = 8.2 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 3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
242 470 124 None -104 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 -104 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 -104 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 -104 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 -104 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
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
11154555 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 800 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
21302490 112805 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 112805 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 112805 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
135398745 2914 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6852400 215937 0 3H-SPIPERONE -794 22 Human 6.2 pKi = 6.2 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-SPIPERONE -794 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
25139331 169928 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL444128 169928 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
3033769 3281 61 3H-RACLOPRIDE -562 19 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3281 61 3H-SPIPERONE -562 19 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3281 61 UNDEFINED -562 19 Human 6.2 pKi = 6.2 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-RACLOPRIDE -562 19 Human 6.2 pKi = 6.2 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-SPIPERONE -562 19 Human 6.2 pKi = 6.2 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 UNDEFINED -562 19 Human 6.2 pKi = 6.2 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-RACLOPRIDE -562 19 Human 6.2 pKi = 6.2 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-SPIPERONE -562 19 Human 6.2 pKi = 6.2 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 UNDEFINED -562 19 Human 6.2 pKi = 6.2 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-RACLOPRIDE -562 19 Human 6.2 pKi = 6.2 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-SPIPERONE -562 19 Human 6.2 pKi = 6.2 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 UNDEFINED -562 19 Human 6.2 pKi = 6.2 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-RACLOPRIDE -562 19 Human 6.2 pKi = 6.2 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-SPIPERONE -562 19 Human 6.2 pKi = 6.2 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 UNDEFINED -562 19 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
44134711 215991 0 3H-Methylspiperone -724 14 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 216130 0 3H-YM 09151-2 -8 5 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 273 6 0 2 4.3 CCCN(CCC)C1C=CC2=C(C1C)C=CC=C2OC None
25139481 184840 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
CHEMBL485227 184840 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
25139477 184245 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL483593 184245 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
44123782 189600 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL514747 189600 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
2477 745 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2389 3331 118 3H-SPIPERONE -22 67 Human 8.2 pKi = 8.2 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-SPIROPERIDOL -22 67 Human 8.2 pKi = 8.2 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-SPIPERONE -22 67 Human 8.2 pKi = 8.2 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-SPIROPERIDOL -22 67 Human 8.2 pKi = 8.2 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-SPIPERONE -22 67 Human 8.2 pKi = 8.2 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-SPIROPERIDOL -22 67 Human 8.2 pKi = 8.2 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-SPIPERONE -22 67 Human 8.2 pKi = 8.2 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-SPIROPERIDOL -22 67 Human 8.2 pKi = 8.2 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-SPIPERONE -22 67 Human 8.2 pKi = 8.2 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-SPIROPERIDOL -22 67 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1212 1662 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2274 3173 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1621 2429 17 None -64 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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 -64 45 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
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
2105 3054 37 None -48 33 Human 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 -48 33 Human 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 -48 33 Human 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 -48 33 Human 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 -48 33 Human 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
2407 3372 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 3372 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 3372 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 3372 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 3372 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
115237 55585 119 None -83 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 None -83 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
242 470 124 None -87 51 Rat 8.1 pKi = 8.1 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 -87 51 Rat 8.1 pKi = 8.1 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 -87 51 Rat 8.1 pKi = 8.1 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 -87 51 Rat 8.1 pKi = 8.1 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 -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
37 778 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 778 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 778 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 778 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 778 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
135398745 2914 112 None -7 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 -7 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 -7 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 -7 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
2865 4143 73 None -66 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 -66 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 -66 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 -66 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 -66 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
49831411 217746 0 None -1 15 Rat 8.1 pKi = 8.1 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
49831411 217746 0 None -1 15 Human 8.1 pKi = 8.1 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
214 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
103 4153 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 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
191 403 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2389 3331 118 3H-SPIPERONE -30 67 Rat 8.1 pKi = 8.1 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-SPIPERONE -30 67 Rat 8.1 pKi = 8.1 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-SPIPERONE -30 67 Rat 8.1 pKi = 8.1 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-SPIPERONE -30 67 Rat 8.1 pKi = 8.1 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-SPIPERONE -30 67 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135398737 958 93 None -13 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 -13 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 -13 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 -13 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 -13 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 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 None -1 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
1212 1662 50 None -77 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 -77 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 -77 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 -77 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 -77 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
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
3294 2006 111 None -11 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 -11 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 -11 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 -11 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 -11 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
135398737 958 93 R-SAT -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 R-SAT -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 R-SAT -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 R-SAT -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 R-SAT -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
65750 216446 0 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
2726 919 68 None -8 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 -8 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 -8 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 -8 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 -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1443 2028 34 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 2028 34 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 2028 34 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 2028 34 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 2028 34 None -1 10 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
2448 99323 70 None -13 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99323 70 None -13 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
1613 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2348 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5280343 188275 124 UNDEFINED 1 32 Human 8.1 pKi = 8.1 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 UNDEFINED 1 32 Human 8.1 pKi = 8.1 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 UNDEFINED 1 32 Human 8.1 pKi = 8.1 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
5467 205928 43 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 205928 43 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
16106 118146 34 3H-SPIPERONE 1 12 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 3H-SPIPERONE 1 12 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2435 3590 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
100 3805 58 None -8 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 -8 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 -8 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 -8 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 -8 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
135409468 2035 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
2274 3173 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
15387 45822 55 3H-SPIPERONE -35 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-SPIPERONE -35 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
213 3853 55 3H-NMSP -6 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 3H-NMSP -6 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 3H-NMSP -6 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 3H-NMSP -6 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 3H-NMSP -6 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
6450478 216012 0 3H-SPIPERONE -18 12 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
11954259 215979 0 3H-SPIPERONE -257 43 Rat 7.1 pKi = 7.1 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
5280343 188275 124 3H-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 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-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 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-Methylspiperone -114 32 Rat 5.1 pKi = 5.1 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
44591086 189581 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
CHEMBL514590 189581 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
44395709 174898 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL456429 174898 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL556361 174898 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2389 3331 118 None -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -7 89 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
228 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 445 28 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
1222 1664 49 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 None -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2601 3780 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
4249 78179 34 None -7 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 78179 34 None -7 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
2601 3780 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
2563 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
55 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
91273 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
CHEMBL274047 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
DB12833 3751 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
11978813 721 79 None -10 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 -10 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 -10 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 -10 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 -10 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
52919 14450 48 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1200986 14450 48 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1588 2325 27 None -16 44 Human 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 -16 44 Human 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 -16 44 Human 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 -16 44 Human 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 -16 44 Human 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
1613 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5022 1651 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 1651 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 1651 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 1651 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 1651 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1524 2181 96 None -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
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 -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
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 -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
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 -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
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 -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
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 -4 52 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2780 110529 36 None -4 10 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 110529 36 None -4 10 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
2389 3331 118 UNDEFINED -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 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 -22 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
25058166 215960 0 3H-SPIPERONE -8 27 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 0 3H-SPIPERONE -8 27 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 3331 118 3H-N-Methylspiperone -22 67 Human 8.1 pKi = 8.1 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-N-Methylspiperone -22 67 Human 8.1 pKi = 8.1 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-N-Methylspiperone -22 67 Human 8.1 pKi = 8.1 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-N-Methylspiperone -22 67 Human 8.1 pKi = 8.1 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-N-Methylspiperone -22 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
16363 596 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 596 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 596 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 596 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 596 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 107531 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
16362 3125 71 None -20 30 Human 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 -20 30 Human 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 -20 30 Human 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 -20 30 Human 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 -20 30 Human 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
135398745 2914 112 None -10 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 -10 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 -10 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 -10 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
1222 1664 49 R-SAT -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 R-SAT -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 R-SAT -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 R-SAT -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 R-SAT -14 33 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
15387 45822 55 3H-NEMONAPRIDE -35 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-NEMONAPRIDE -35 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
44591043 176812 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
CHEMBL460855 176812 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
None 216014 0 3H-SPIPERONE -85 3 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 411 6 1 3 3.9 C1CCC(CC1)NC(=O)N2CCN(CC2)CCCC(=O)C3=CC=C(C=C3)F.Cl None
2402 3370 62 3H-SPIPERONE -2 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 3H-SPIPERONE -2 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 3H-SPIPERONE -2 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 3H-SPIPERONE -2 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 3H-SPIPERONE -2 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
10060538 4576 7 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 4576 7 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
None 216431 0 3H-SPIPERONE -467 4 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
681 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 None -2 39 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
135398737 958 93 3H-SPIPERONE -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-SPIPERONE -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-SPIPERONE -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-SPIPERONE -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-SPIPERONE -13 89 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2389 3331 118 3H-SCH23390 -22 67 Human 8.1 pKi = 8.1 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-SCH23390 -22 67 Human 8.1 pKi = 8.1 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-SCH23390 -22 67 Human 8.1 pKi = 8.1 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-SCH23390 -22 67 Human 8.1 pKi = 8.1 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-SCH23390 -22 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2435 3590 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 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-SPIPERONE -10 48 Human 8.1 pKi = 8.1 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-SPIPERONE -10 48 Human 8.1 pKi = 8.1 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-SPIPERONE -10 48 Human 8.1 pKi = 8.1 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-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
3168 9262 92 None -4 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9262 92 None -4 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1712 2492 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1212 1662 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
119570 3159 96 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 None -10 40 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
1238 203174 24 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2726 919 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 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-SPIPERONE -7 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2914 112 3H-SPIPERONE -7 65 Rat 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-SPIPERONE -7 65 Rat 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-SPIPERONE -7 65 Rat 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-SPIPERONE -7 65 Rat 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
2470 3653 50 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 None -20 59 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2726 919 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
191 403 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
None 216431 0 3H-SPIPERONE -467 4 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
164512405 215949 0 3H-SPIPERONE -10 13 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
202478 204687 20 3H-NMSP -7 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 20 3H-NMSP -7 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
115368 3056 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
2112 3056 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
7556 3056 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
CHEMBL1472975 3056 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
DB08922 3056 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
16363 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
312 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
9215 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
CHEMBL297302 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
DB12867 596 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
1577 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 3703 110 None -10 21 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
3033769 3281 61 None -288 19 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
3299 3281 61 None -288 19 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
94 3281 61 None -288 19 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
CHEMBL8809 3281 61 None -288 19 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
DB12518 3281 61 None -288 19 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
16094676 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
8439 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
CHEMBL219182 232 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
2274 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
31101 729 40 None -186 36 Human 6.4 pKi = 6.4 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 12388666
35 729 40 None -186 36 Human 6.4 pKi = 6.4 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 12388666
403 729 40 None -186 36 Human 6.4 pKi = 6.4 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 12388666
CHEMBL493 729 40 None -186 36 Human 6.4 pKi = 6.4 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 12388666
DB01200 729 40 None -186 36 Human 6.4 pKi = 6.4 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 12388666
1577 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
1577 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
2537 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5355 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5501 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
643497 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
688272 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
958 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
960 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL196677 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL26 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL267044 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB00391 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB16021 3703 110 None -10 21 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2407 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
59227 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
941 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
CHEMBL1303 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
DB05271 3372 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
214 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
2740 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
5566 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
66064 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
CHEMBL422 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
DB00831 3860 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
103 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 4153 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
72737723 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
8440 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
CHEMBL3335556 2578 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
2 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
2 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
2 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
54562 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
54562 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
54562 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
CHEMBL240773 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
CHEMBL240773 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
CHEMBL240773 3261 23 None -2 29 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
681 1465 72 None -2 39 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
940 1465 72 None -2 39 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
947 1465 72 None -2 39 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
CHEMBL59 1465 72 None -2 39 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
DB00988 1465 72 None -2 39 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
3251 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
5684 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
80 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
CHEMBL31354 4072 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
10425450 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
10425450 201 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 201 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 201 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 201 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
1613 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
205 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
3964 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
CHEMBL831 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
DB00408 2348 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
228 445 28 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 445 28 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 445 28 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 445 28 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 445 28 None -1 24 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
2435 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
2435 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
2435 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
60149 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
60149 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
60149 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
98 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
98 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
98 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
CHEMBL12713 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
CHEMBL12713 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
CHEMBL12713 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
DB06144 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
DB06144 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
DB06144 3590 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
133008 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
3302 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
CHEMBL444309 2242 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
1353 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
1353 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
1353 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3559 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
3559 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
3559 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
86 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
86 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
86 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
CHEMBL54 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
CHEMBL54 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
CHEMBL54 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
DB00502 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
DB00502 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
DB00502 1911 93 None -3 83 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3645619 3034 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
975 3034 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
CHEMBL45244 3034 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
11301655 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
8441 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
CHEMBL127257 200 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
133079 3638 42 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
980 3638 42 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
CHEMBL69759 3638 42 None 1 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
5615 3899 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
5781 3899 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
CHEMBL1179189 3899 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
3303 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
5311200 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
CHEMBL267014 2244 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
179 400 115 None -50 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 -50 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 -50 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 -50 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 -50 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
243 3202 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
213 3853 55 None -6 44 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 None -6 44 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 None -6 44 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 None -6 44 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 None -6 44 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2342 599 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
331 599 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
7124 599 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
CHEMBL1201250 599 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
DB00767 599 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
5281878 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1660 35 None -14 17 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11976 920 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
5567 42802 27 None -11 8 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42802 27 None -11 8 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
6603897 2247 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
978 2247 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
CHEMBL60518 2247 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
37459 746 13 None -123 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
62 746 13 None -123 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
CHEMBL8514 746 13 None -123 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
3408722 2714 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
44 2714 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
CHEMBL286252 2714 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
1153 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
12668023 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026874 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026875 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
3341 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
6603851 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
933 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
939 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
985 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1160786 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1161520 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL588 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
DB00800 1628 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
2202 3132 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 3132 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 3132 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 3132 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 3132 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
57267 1593 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
966 1593 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
CHEMBL8946 1593 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
DB15492 1593 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
2105 3054 37 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3054 37 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3054 37 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3054 37 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3054 37 None -48 33 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
242 470 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
34 470 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
60795 470 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
CHEMBL1112 470 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
DB01238 470 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
37 778 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 778 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 778 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 778 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 778 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
681 1465 72 None -7 39 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
940 1465 72 None -7 39 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
947 1465 72 None -7 39 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
CHEMBL59 1465 72 None -7 39 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
DB00988 1465 72 None -7 39 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
135398737 958 93 None -13 89 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
38 958 93 None -13 89 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
722 958 93 None -13 89 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
CHEMBL42 958 93 None -13 89 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
DB00363 958 93 None -13 89 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
2726 919 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
621 919 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
83 919 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
CHEMBL71 919 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
DB00477 919 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
11429930 3341 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
982 3341 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
2601 3780 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 3780 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 3780 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 3780 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 3780 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
219050 3373 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3373 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3373 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
1588 2325 27 None -16 44 Human 8.3 pKi None 8.3 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 12388666
28864 2325 27 None -16 44 Human 8.3 pKi None 8.3 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 12388666
43 2325 27 None -16 44 Human 8.3 pKi None 8.3 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 12388666
CHEMBL157138 2325 27 None -16 44 Human 8.3 pKi None 8.3 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 12388666
DB00589 2325 27 None -16 44 Human 8.3 pKi None 8.3 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 12388666
133079 3638 42 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
980 3638 42 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
CHEMBL69759 3638 42 None -1 4 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
10336538 1625 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
974 1625 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
CHEMBL310843 1625 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
2470 3653 50 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
3300 3653 50 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
5265 3653 50 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
99 3653 50 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
CHEMBL267930 3653 50 None -20 59 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
973 1177 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
9796720 1177 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
CHEMBL77395 1177 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
977 1178 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
9820261 1178 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
CHEMBL66227 1178 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
188942 2818 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
3297 2818 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
979 2818 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
CHEMBL103772 2818 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
5041 3294 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
981 3294 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
CHEMBL4096543 3294 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188