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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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44417940 81694 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81694 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
137644041 158449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 158449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
137644041 158449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 158449 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
10150552 81593 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81593 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417944 141810 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141810 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417894 80584 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80584 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417921 81125 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 81125 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417925 81464 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81464 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417875 80794 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80794 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417823 165772 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165772 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141768 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141768 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
44207909 16699 3 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16699 3 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16699 3 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16699 3 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
15133403 206350 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 206350 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018999 81119 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 81119 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018957 82442 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82442 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141560 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141560 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417998 82395 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 82395 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018944 82208 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 82208 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417962 82086 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 82086 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417846 82099 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 82099 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25110804 95490 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95490 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44454966 155426 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 155426 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44417917 82096 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 82096 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418009 81863 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81863 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 82300 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 82300 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44455444 95045 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 95045 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455414 97418 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 97418 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455417 97461 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 97461 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
24952417 91515 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91515 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952419 91525 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91525 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417867 141513 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 141513 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018896 141694 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141694 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
10150954 141547 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141547 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24808474 91522 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91522 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417956 96651 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96651 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417947 141511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 141511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
10310316 81120 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 81120 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24952765 91527 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91527 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10173787 82438 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82438 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018932 80306 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 80306 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417843 81961 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81961 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417886 141698 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141698 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 169019 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 169019 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455368 95630 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95630 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952418 91517 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91517 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135478 91519 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91519 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135482 91523 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91523 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135474 91524 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91524 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
22018997 141708 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141708 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417992 82457 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82457 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10173726 80845 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80845 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417857 141656 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141656 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150955 80919 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80919 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417888 80405 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 80405 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417999 82206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 82206 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018856 80607 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80607 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
44417995 82441 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82441 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417847 82435 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82435 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417821 80559 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80559 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
10126754 81557 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81557 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455443 95711 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95711 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952056 91518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141886 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141886 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018945 141723 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141723 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417966 161518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 161518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018914 80915 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80915 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
59135486 91521 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91521 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417975 141860 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141860 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141797 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141797 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417838 81597 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81597 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417877 81137 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 81137 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135492 91526 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91526 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417911 82439 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82439 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417915 141389 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 141389 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
24952055 91520 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91520 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141886 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141886 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417845 141886 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141886 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417864 80290 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 80290 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417979 82146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 82146 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417948 141749 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141749 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44455367 95629 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95629 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
59135471 91513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91513 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417973 141475 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 141475 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417844 141587 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141587 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141661 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141661 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417982 82512 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82512 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417848 141622 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141622 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417832 141752 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141752 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417976 165942 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165942 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417959 81795 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81795 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018964 141670 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141670 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44418003 82468 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82468 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417873 81459 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81459 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44418002 82565 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82565 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
9799244 80585 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80585 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141817 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141817 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417856 80840 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80840 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
11994411 1004 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
1306 1004 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
CHEMBL214523 1004 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
4033 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
9826520 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
CHEMBL214957 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
4033 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
9826520 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
CHEMBL214957 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
10004545 74952 7 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11995648 82398 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
CHEMBL217269 82398 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
11994912 82891 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
CHEMBL218077 82891 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
10004545 74952 7 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10004545 74952 7 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11994412 141711 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
CHEMBL385690 141711 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
11993893 141823 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
CHEMBL386349 141823 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
11995024 141434 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL384133 141434 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
11995242 80817 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
CHEMBL215235 80817 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
44416336 80063 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
CHEMBL213008 80063 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
44442095 94302 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 94302 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11994413 80520 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
CHEMBL214806 80520 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
11994784 82292 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL217178 82292 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
11994786 82592 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
CHEMBL217887 82592 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
10004545 74952 7 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44416314 79965 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212657 79965 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11994913 80554 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
CHEMBL214871 80554 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
11994659 81551 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
CHEMBL216117 81551 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
11993894 82563 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217843 82563 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
11994780 82510 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
CHEMBL217733 82510 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
11995244 80575 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214944 80575 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
44416857 80242 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
CHEMBL213813 80242 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
11553871 81117 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL215643 81117 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
44416316 169286 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL441368 169286 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416837 141540 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384724 141540 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
10225681 80338 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214276 80338 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414475 78075 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 78075 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44417150 80233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213766 80233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416976 81476 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL216005 81476 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
23027411 198520 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 198520 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44430471 86806 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86806 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430460 87226 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 87226 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
44430463 149399 1 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 149399 1 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
70688018 74843 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74843 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436085 74888 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74888 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44394824 124268 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 124268 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
10025637 65584 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65584 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44416751 82120 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
CHEMBL216649 82120 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
44416350 141951 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL387195 141951 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485029 198493 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577714 198493 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
54581468 60585 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760068 60585 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
45267576 196632 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 196632 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
70687479 73510 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73510 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57402044 68844 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922251 68844 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
23532179 68846 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922253 68846 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57395050 68856 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68856 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44394800 122356 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 122356 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123631 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123631 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 131452 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 131452 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11189610 165777 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165777 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
20817821 76859 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76859 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
23120540 196139 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 196139 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031907 139126 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786923 139126 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
57398576 68842 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922249 68842 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57402045 68845 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922252 68845 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
10202381 68858 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68858 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44418006 82410 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217349 82410 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973799 82462 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82462 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11188955 80467 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80467 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
3114950 37769 32 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37769 32 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
54586331 60584 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760065 60584 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
11526309 189218 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 189218 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
44417983 82160 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216935 82160 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70689520 73466 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73466 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11837128 72130 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 72130 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
44562404 176964 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176964 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
44410878 78108 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 78108 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
44592257 178991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470840 178991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
58062385 125877 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
CHEMBL3648387 125877 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
4062524 32622 7 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
CHEMBL1412874 32622 7 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
46846317 59153 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
CHEMBL1699198 59153 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
46846319 59208 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
CHEMBL1701679 59208 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
24856242 35301 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
CHEMBL1436519 35301 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
49866089 16245 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16245 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44405481 71850 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71850 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691720 73553 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73553 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
23120586 196737 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 196737 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
2729098 80495 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80495 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
11563383 70515 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70515 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
52917998 60632 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60632 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430477 87218 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 87218 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430476 152306 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 152306 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
23593464 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436117 74893 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74893 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
53324076 56709 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56709 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
21108056 68080 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 68080 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391028 68085 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 68085 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9910346 64732 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64732 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10070016 71463 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
CHEMBL196208 71463 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
11775399 63360 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63360 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11495754 71932 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71932 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57404360 73147 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011534 73147 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
49865653 16042 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 16042 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865678 16060 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 16060 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
10183297 93312 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 93312 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
44394909 67034 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 67034 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44394856 66134 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 66134 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
46850893 59723 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
CHEMBL1723963 59723 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
46172926 59338 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1706758 59338 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46861572 125866 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
CHEMBL3648376 125866 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
46172933 59864 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
CHEMBL1729376 59864 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
3247171 23329 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
CHEMBL1332346 23329 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
23603500 21827 7 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
CHEMBL1319565 21827 7 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
49866035 16230 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16230 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417961 82077 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216564 82077 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394866 124349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 124349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
16438224 52293 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
CHEMBL1589201 52293 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
54580459 60583 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760063 60583 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
46846318 59641 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1720892 59641 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
58062375 125884 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
CHEMBL3648394 125884 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
44394807 66218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 66218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44405646 96873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
70691649 73455 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73455 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
58062307 125870 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
CHEMBL3648380 125870 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
11562129 71077 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 71077 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562442 179189 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 179189 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
58062320 125865 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648375 125865 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
46188959 121762 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589135 121762 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
44442151 94006 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 94006 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
2810388 42498 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
CHEMBL1499675 42498 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
44414520 80271 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 80271 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
11547011 141614 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141614 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
11610423 166019 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 166019 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
52918016 60646 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60646 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436082 74890 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74890 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689612 73604 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73604 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11635674 201849 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 201849 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
11496313 72312 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 72312 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416956 80245 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213824 80245 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416995 83092 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL218186 83092 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
44416348 81235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215862 81235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414589 80164 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 80164 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45484995 198519 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 198519 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11713742 93563 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93563 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11570031 73498 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73498 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44397202 67224 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 67224 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
127032787 139158 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787237 139158 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
10319824 67081 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 67081 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
46835812 59531 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1716158 59531 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
5810215 26404 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
CHEMBL1359426 26404 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
45269336 195982 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 195982 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
58062364 125868 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
CHEMBL3648378 125868 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
5091342 51798 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
CHEMBL1585038 51798 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
45273642 196455 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 196455 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44562545 189103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 189103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
46835786 59591 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
CHEMBL1718965 59591 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
58062388 125863 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
CHEMBL3648373 125863 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
44416363 80375 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214427 80375 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
1479656 59787 15 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
CHEMBL1726382 59787 15 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
24856245 46130 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
CHEMBL1533829 46130 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
2982342 55158 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1342885 55158 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1617311 55158 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
11995644 82368 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217228 82368 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416297 96978 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL266415 96978 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44394592 65762 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65762 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
45382326 59838 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1728485 59838 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
16191617 50735 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
CHEMBL1576145 50735 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
44442153 94047 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 94047 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
46835820 59814 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1727473 59814 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
2386953 55268 2 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1339438 55268 2 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1618129 55268 2 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
23027035 198547 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 198547 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
11583049 141948 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141948 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
44430459 87164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 87164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
16718619 121765 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589154 121765 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
70691736 73601 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73601 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693807 73602 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73602 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10369833 92567 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92567 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
44414481 138900 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138900 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54580457 60579 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60579 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10456385 92140 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 92140 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
44394606 67253 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 67253 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397008 66902 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66902 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
16756405 92867 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92867 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
9955811 66171 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 66171 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
10377822 126824 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126824 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
135519896 72098 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
CHEMBL1977747 72098 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
90666255 109365 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 109365 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
3338232 39441 8 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
CHEMBL1471999 39441 8 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
22254604 123876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
952248 46558 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
CHEMBL1537947 46558 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
46846336 59783 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1726190 59783 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
11592099 93502 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93502 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
44410904 172457 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 172457 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11974131 141986 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141986 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
90666251 109361 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 109361 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45382325 59457 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
CHEMBL1712328 59457 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
44405431 71951 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71951 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
46892535 125862 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
CHEMBL3648372 125862 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
54579973 60642 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60642 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436120 74879 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74879 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
70693734 73477 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73477 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687551 73617 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73617 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70691738 73622 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73622 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
24857598 19121 16 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 19121 16 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11655872 71717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
10027853 71862 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71862 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
50908737 19137 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 19137 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
54587368 60588 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760077 60588 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
57404359 73144 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011528 73144 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
127033672 139021 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785819 139021 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690365 138175 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 138175 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
16755969 92315 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 92315 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394764 123169 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 123169 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
9895868 69582 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69582 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
16756640 93278 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 93278 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
11994910 80414 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL214571 80414 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
70681198 73573 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73573 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46850887 59698 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
CHEMBL1723067 59698 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
49865868 16176 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 16176 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062381 125864 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648374 125864 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
58062316 125873 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648383 125873 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
10255474 123671 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123671 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
11510669 189299 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 189299 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70693795 73559 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73559 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45382320 59994 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
CHEMBL1734525 59994 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
70687470 73461 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73461 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865977 16218 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16218 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062334 125867 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648377 125867 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
58062344 125880 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
CHEMBL3648390 125880 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
70691333 77972 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77972 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
135693566 23763 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
CHEMBL1335685 23763 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
11539632 70561 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70561 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44414432 77938 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77938 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666094 109327 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 109327 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430468 92361 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 92361 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
127031622 139190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787639 139190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11511776 189300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 189300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70681213 73603 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73603 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11520239 3632 11 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3632 11 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3632 11 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
4219492 71437 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71437 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44417043 81372 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215932 81372 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
44417067 141992 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387438 141992 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
54584908 60639 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760242 60639 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
127031909 139152 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787166 139152 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
70685336 73454 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73454 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394683 67208 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 67208 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46850894 59360 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1707830 59360 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
2827417 54508 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
CHEMBL1609915 54508 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
3732471 38888 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
CHEMBL1467280 38888 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
54585833 60622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760222 60622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
54585862 60630 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760230 60630 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
49865654 16043 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 16043 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70689526 73507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
1129890 56157 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1578660 56157 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1625981 56157 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
70681116 73463 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73463 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44416255 80049 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212963 80049 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
2766793 50078 14 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
CHEMBL1569862 50078 14 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
4439874 51487 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
CHEMBL1582511 51487 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
46835815 59319 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
CHEMBL1705920 59319 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
2709719 26413 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
CHEMBL1359489 26413 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
23027245 197128 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 197128 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
11683903 82429 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82429 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
71226964 129181 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 129181 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11599186 73499 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73499 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
16718619 121765 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121765 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
4033 1899 48 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1899 48 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1899 48 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
60150483 73552 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73552 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70685409 73608 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73608 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11583744 71724 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71724 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10005009 166376 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 166376 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54586330 60580 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760060 60580 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
11374857 80219 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 80219 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
70681114 73459 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73459 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
54582960 60633 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760235 60633 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394639 66706 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66706 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948187 52877 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
CHEMBL1595687 52877 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
20854116 25424 7 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
CHEMBL1350024 25424 7 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
11611530 134805 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134805 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
70695853 73469 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73469 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553316 71634 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71634 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
45269335 196463 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 196463 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
11155432 82487 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82487 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
16190353 24693 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
CHEMBL1343746 24693 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
786990 51983 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
CHEMBL1586617 51983 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
11640515 80509 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80509 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11640515 80509 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80509 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
22254551 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254551 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
22254551 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 125044 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
17596249 33304 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
CHEMBL1418691 33304 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
10041636 123195 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 123195 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
21940008 64725 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64725 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64732 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64732 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56708 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56708 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11505089 194807 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 194807 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
70685407 73600 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73600 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
54585377 60589 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760078 60589 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54585378 60590 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760079 60590 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54582958 60626 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760226 60626 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70695929 73615 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73615 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394959 67210 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 67210 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394907 165992 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165992 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
46172924 59618 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
CHEMBL1720022 59618 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
1479652 51729 15 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51729 15 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46172940 59597 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
CHEMBL1719118 59597 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
11974230 166012 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 166012 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
800280 46682 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
CHEMBL1539046 46682 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
58062315 125878 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
CHEMBL3648388 125878 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
22254571 66969 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66969 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
46172927 59730 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
CHEMBL1724285 59730 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
53317307 56712 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56712 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
44438741 93824 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93824 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
660602 55179 9 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1314041 55179 9 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1617460 55179 9 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
58062386 125881 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
CHEMBL3648391 125881 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
44417883 80364 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL214383 80364 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
89691096 139477 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 139477 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
23593474 64703 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64703 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11559625 56715 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56715 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687473 73474 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73474 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685410 73611 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73611 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46933537 16063 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 16063 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417850 81657 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81657 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
57391574 68853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922260 68853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
57403783 68854 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922261 68854 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
46850892 60016 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1735215 60016 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
70695854 73470 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73470 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44388559 60719 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60719 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44417970 98223 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL274326 98223 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70695916 73570 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73570 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405518 140359 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 140359 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46172915 59525 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1715946 59525 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
24892611 55892 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1538063 55892 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1623531 55892 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
49865928 16195 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16195 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
12005269 40217 6 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
CHEMBL1480448 40217 6 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
11560917 124052 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 124052 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44405519 72371 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72371 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11995343 80424 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214604 80424 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
1314 3727 21 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
9865843 3727 21 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
CHEMBL178707 3727 21 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
56598528 139070 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786350 139070 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690574 138325 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 138325 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
24780883 56713 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56713 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
44557554 196411 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 196411 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
70681217 73620 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73620 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11705240 132813 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132813 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416871 80497 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214733 80497 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416296 80376 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214429 80376 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
16755970 92314 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 92314 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
16756284 151486 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 151486 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
44394572 66514 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66514 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405415 72569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
11975326 80508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
58062298 125879 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
CHEMBL3648389 125879 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
44410944 77052 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 77052 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394855 67280 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 67280 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
135515070 21128 2 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
CHEMBL1312413 21128 2 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
11464405 80496 26 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80496 26 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
70687537 73551 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73551 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
58062333 125869 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648379 125869 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
44438748 149497 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 149497 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11842385 38131 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
CHEMBL1461182 38131 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
44416232 80099 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL213154 80099 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995025 168841 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
CHEMBL437914 168841 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
11993892 141617 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
CHEMBL385171 141617 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
9821717 198538 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL578049 198538 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522703 76376 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76376 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
16006978 80073 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 80073 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11995347 80907 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
CHEMBL215286 80907 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
23027806 197207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
CHEMBL568208 197207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
18436094 74885 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74885 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994660 96553 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
CHEMBL262945 96553 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
23027679 198546 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578166 198546 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44417021 80493 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214716 80493 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416337 80373 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214416 80373 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
18436038 76374 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76374 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
11994911 141988 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
CHEMBL387419 141988 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
9932896 74527 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74527 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
57398088 68082 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 68082 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9932896 74527 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74527 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
45485062 197168 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 197168 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
57521365 2615 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2615 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2615 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
44414309 138889 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138889 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL472083 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL534717 179144 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
23120512 195308 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 195308 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
24963343 73149 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 73149 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
16739324 149759 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149759 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
71226400 129183 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 129183 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 139068 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 139068 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
127031338 139072 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 139072 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
71226277 139119 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 139119 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57403784 68855 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68855 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23532181 68857 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922266 68857 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
70681214 73606 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73606 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44469273 197558 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 197558 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10436090 66206 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 66206 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394609 123885 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123885 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
44394792 124740 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124740 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
16659240 82214 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217079 82214 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
22348155 76585 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76585 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
22348261 77063 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 77063 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
22348066 165830 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165830 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
11995141 81154 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL215782 81154 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
45485004 198440 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL577259 198440 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
127033096 139179 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787492 139179 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57393331 68847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922254 68847 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57391572 68848 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922255 68848 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
16756637 93203 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 93203 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
46835808 59428 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
CHEMBL1710711 59428 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
30979231 69526 4 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934102 69526 4 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
46846334 59516 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1715364 59516 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
3527724 50487 2 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
CHEMBL1573548 50487 2 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
54584904 60625 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760225 60625 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
11546687 81555 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81555 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
5129939 36335 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
CHEMBL1446321 36335 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
58062355 125871 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
CHEMBL3648381 125871 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
10024171 188045 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 188045 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
56597689 139166 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 139166 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11599973 194897 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 194897 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
70681216 73613 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73613 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45484984 197259 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568458 197259 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
10083869 65574 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65574 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46835819 59304 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
CHEMBL1705448 59304 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
10083869 65574 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11545677 70377 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70377 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417974 97042 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL266972 97042 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11974233 82142 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 82142 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
1082177 25880 6 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
CHEMBL1353612 25880 6 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
90666098 109331 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 109331 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45273659 195832 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 195832 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44394604 125050 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 125050 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
1933024 26320 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
CHEMBL1358809 26320 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
44143495 184255 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 184255 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
127030069 139108 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 139108 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597988 139153 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 139153 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317306 56705 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56705 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53325164 56717 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56717 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
57392823 68081 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 68081 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
10000146 64647 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64647 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
127033673 139099 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786609 139099 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
23593472 64705 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64705 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70695915 73567 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73567 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394611 124347 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 124347 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 124347 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 124347 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
54584906 60637 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760239 60637 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46172941 59562 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1717450 59562 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
675719 41846 17 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
CHEMBL1493564 41846 17 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
58062312 125872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
CHEMBL3648382 125872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
44394799 66254 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 66254 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
70695913 73549 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73549 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
2849164 55851 29 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1518183 55851 29 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1623233 55851 29 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
58062371 125874 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
CHEMBL3648384 125874 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
22254582 66972 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66972 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
2963624 36499 7 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
CHEMBL1447678 36499 7 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
44430455 86852 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86852 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430475 87070 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 87070 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
49801837 139010 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 139010 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597851 139060 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 139060 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 139161 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 139161 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89691439 138248 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 138248 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53320117 56722 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56722 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
11654412 198918 26 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 198918 26 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70695918 73575 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73575 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
25017033 19286 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19286 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
45485018 198611 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578784 198611 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
70691723 73566 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73566 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756754 92129 27 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 92129 27 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
54583912 60596 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760085 60596 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
44442063 94395 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 94395 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24818378 29651 4 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
CHEMBL1386141 29651 4 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
1479652 51729 15 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51729 15 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
653550 37141 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
CHEMBL1452812 37141 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
646509 24807 7 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
CHEMBL1344766 24807 7 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
44414391 80197 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 80197 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414540 80326 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 80326 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
11994138 141647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL385347 141647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
54585863 60643 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60643 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89702226 139313 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 139313 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11596311 56716 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56716 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70691722 73565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
9806086 65207 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 65207 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
16756403 150943 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150943 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
46188603 121764 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121764 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
44417977 82296 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217193 82296 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
3825639 29829 16 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
CHEMBL1387472 29829 16 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
44394864 126198 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 126198 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948210 38415 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
CHEMBL1463698 38415 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
2424660 40400 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
CHEMBL1482022 40400 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
70695851 73452 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73452 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45487653 199007 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 199007 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11994137 82564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL217844 82564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
23027830 197292 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568664 197292 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
54579974 3240 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3240 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3240 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
127030071 139177 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 139177 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691652 73472 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73472 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442065 94311 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 94311 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
11628328 195539 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 195539 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
16755871 92495 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92495 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44417941 96590 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL263171 96590 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11511219 66135 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 66135 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416828 141743 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385883 141743 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44416949 141793 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL386188 141793 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416272 80024 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212883 80024 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416212 80922 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215334 80922 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
54583953 60624 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760224 60624 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
9824428 66257 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 66257 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44416975 141830 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL386397 141830 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
44405560 72448 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72448 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
16192403 38576 3 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
CHEMBL1464847 38576 3 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
70685397 73564 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73564 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695917 73572 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73572 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46892401 125883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
CHEMBL3648393 125883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
90666257 109367 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 109367 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45485002 198521 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577913 198521 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11222404 195378 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 195378 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031356 139191 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 139191 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70685398 73576 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73576 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687550 73614 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73614 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756185 149721 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149721 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
20817761 77268 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 77268 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
90666252 109362 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 109362 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10434776 126382 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 126382 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11653882 141305 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 141305 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
54581980 60592 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760081 60592 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
16756639 93230 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 93230 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
46850889 59555 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1717204 59555 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
54586826 60631 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760231 60631 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2310853 56213 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1335094 56213 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1626478 56213 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
11510887 82269 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 82269 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
52918017 60647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60647 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44143496 192087 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 192087 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
56597542 138951 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138951 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 139170 27 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 139170 27 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11502008 56572 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56572 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70689525 73506 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73506 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693808 73619 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73619 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756073 92288 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 92288 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10324628 142225 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 142225 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 167363 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 167363 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
45487384 196841 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 196841 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
44438755 93503 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93503 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
44394591 122658 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122658 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
16756401 150942 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150942 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
46172921 59344 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
CHEMBL1706988 59344 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
2649486 29957 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
CHEMBL1388448 29957 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
11974227 169305 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 169305 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
2491454 46850 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
CHEMBL1540447 46850 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
127031621 139095 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786572 139095 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
16665072 98538 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98538 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
10047339 70405 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70405 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10250850 72411 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72411 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44403765 135860 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135860 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
49865976 16217 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16217 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11282448 62575 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62575 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
16193698 33073 4 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
CHEMBL1416734 33073 4 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
11994662 141514 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL384553 141514 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
23120575 195873 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 195873 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44430452 149758 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149758 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
56598130 139150 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 139150 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
21939915 64716 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64716 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9983233 76001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 76001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348022 77351 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 77351 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
44394569 66217 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 66217 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405618 72015 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 72015 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
46172934 59232 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1702876 59232 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
46846323 59932 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1731906 59932 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
44438753 93460 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93460 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
58062362 125861 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
CHEMBL3648371 125861 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
70681115 73460 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73460 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
1431538 29202 5 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
CHEMBL1382150 29202 5 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
3229425 51644 3 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
CHEMBL1583768 51644 3 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
90666095 109328 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 109328 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
90666096 109329 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 109329 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10258364 194784 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
70693733 73475 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73475 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46933538 16216 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16216 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10360874 64934 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64934 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11994414 80316 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
CHEMBL214181 80316 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
11995342 80521 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL214808 80521 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
11995245 80587 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214991 80587 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
44416890 80490 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214705 80490 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44417044 81238 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215868 81238 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416377 81094 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215565 81094 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995444 80463 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214663 80463 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11994017 81003 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215364 81003 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
57522946 76386 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76386 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
11994019 141657 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
CHEMBL385391 141657 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
57522947 76387 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76387 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11995442 82277 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
CHEMBL217159 82277 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
11995345 141548 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
CHEMBL384770 141548 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
11995344 80598 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL215039 80598 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
18436119 76382 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76382 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44416875 80385 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214476 80385 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44414357 79753 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79753 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030367 139063 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 139063 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317305 56704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56704 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70693732 73462 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73462 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683287 73571 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73571 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394922 66141 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 66141 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394726 66159 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 66159 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394860 66248 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 66248 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10361342 122924 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122924 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10248906 123653 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123653 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
9828622 96654 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
CHEMBL263702 96654 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
45279489 123580 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123580 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
49865975 16215 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16215 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
135478067 23871 15 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
135485243 23871 15 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
154780186 23871 15 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
CHEMBL1336601 23871 15 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
70687471 73468 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73468 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45273887 121763 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
CHEMBL3589138 121763 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
11974030 155276 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 155276 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11995646 80280 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL213966 80280 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
54582957 60623 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760223 60623 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430453 87922 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87922 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
70681113 73456 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73456 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687549 73610 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73610 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70681215 73612 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73612 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693810 73625 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73625 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10075375 76002 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 76002 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11994275 82414 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
CHEMBL217356 82414 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
44417140 80254 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL213864 80254 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416851 141842 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
CHEMBL386460 141842 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
44416858 166104 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL425982 166104 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
54581466 60573 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760003 60573 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
24997711 59220 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
CHEMBL1702161 59220 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
46835796 59248 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
CHEMBL1703306 59248 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
46846326 59368 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708047 59368 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846335 59396 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1709509 59396 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172916 59638 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1720787 59638 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
44417986 166074 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425801 166074 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394573 123682 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123682 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
54579972 60641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760244 60641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
44417968 81576 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216241 81576 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416303 138667 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL377758 138667 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
4881730 51897 5 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
CHEMBL1585808 51897 5 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
54580923 60593 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760082 60593 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
70695855 73476 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73476 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11712898 179188 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 179188 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70687538 73574 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73574 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756641 142589 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142589 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
54585827 60594 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760083 60594 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
6463414 47186 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
CHEMBL1543278 47186 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
44414571 80275 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 80275 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
21062998 64715 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64715 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798744 139473 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 139473 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
70691650 73458 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73458 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693737 73505 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73505 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57391573 68850 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922257 68850 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46846325 59201 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1701512 59201 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846316 59381 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708651 59381 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
24794275 23768 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
CHEMBL1335692 23768 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
16191953 52311 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
CHEMBL1589399 52311 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
90666259 109369 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 109369 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
56597407 139054 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 139054 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
123471111 139138 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 139138 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53318801 56701 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56701 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
21108114 68074 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 68074 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
70695930 73618 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73618 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
70693809 73623 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73623 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
10437982 92571 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92571 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
22348219 76524 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76524 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
21062991 64701 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64701 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70685395 73546 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73546 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44394644 66136 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 66136 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405487 71875 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71875 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46850891 59181 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
CHEMBL1700476 59181 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
10480652 65321 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 65321 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
10332650 66194 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 66194 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
44414392 80198 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 80198 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030368 138977 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138977 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
44442144 154695 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154695 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70691725 73577 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73577 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70683300 73609 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73609 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44414542 80335 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 80335 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54582015 60629 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760229 60629 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683237 73453 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73453 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70681117 73465 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73465 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
16756642 93279 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 93279 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44405464 166351 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 166351 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
46846321 59738 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1724571 59738 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
935062 46438 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1536967 46438 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
11995140 141478 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384371 141478 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
54582476 60591 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
CHEMBL1760080 60591 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
16756753 92128 1 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 92128 1 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
44394605 67018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 67018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11993897 97385 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL269695 97385 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
90666262 109373 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 109373 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
9844702 64707 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64707 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
49866036 16231 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16231 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
46850890 59119 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
CHEMBL1698073 59119 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
46172918 59413 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
CHEMBL1710128 59413 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
11995026 141907 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
CHEMBL386900 141907 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
44405408 72434 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72434 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44397221 67132 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 67132 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
54585376 60587 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760071 60587 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
70693620 73145 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011529 73145 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
69603769 73450 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73450 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70695859 73502 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73502 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
90666261 109372 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 109372 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70685408 73605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
11974231 82420 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 82420 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
46835791 59356 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1707743 59356 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46172919 59856 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
CHEMBL1729021 59856 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
46172935 59965 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1733129 59965 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
11995137 141557 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384825 141557 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416362 165774 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL424723 165774 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485063 197368 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL569204 197368 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522945 76385 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76385 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
70691653 73481 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73481 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687477 73500 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73500 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11561126 68861 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68861 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44417949 82290 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217171 82290 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
18436114 74892 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74892 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
18435902 76375 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76375 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57523087 1158 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1158 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1158 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
23027211 197250 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 197250 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
21939937 64717 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64717 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11995552 80282 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL213973 80282 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995138 82276 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217158 82276 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
56597991 139176 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 139176 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
10159452 74844 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74844 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689594 73547 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73547 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394891 65215 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 65215 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
57400241 68849 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922256 68849 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
70687361 73146 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
CHEMBL2011532 73146 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
46835788 59900 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1730555 59900 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
70685346 73497 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73497 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44438745 93858 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93858 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414342 78036 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 78036 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54583954 60635 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60635 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394826 66605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
11440762 82141 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 82141 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
11531660 135594 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135594 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
54585375 60586 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760070 60586 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
46835793 59306 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
CHEMBL1705499 59306 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
11973801 141968 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141968 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
90666254 109364 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 109364 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
70691724 73569 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73569 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11995346 81490 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL216008 81490 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11974228 80372 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 80372 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
71816518 138284 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 138284 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442097 94010 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 94010 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44417862 80631 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80631 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
22348140 168723 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168723 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
11648240 71461 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71461 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
16739263 93414 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 93414 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
90666264 109375 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 109375 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127031339 139175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787457 139175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
1314 3727 21 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3727 21 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3727 21 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
23593468 64704 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64704 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70683299 73607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44414310 138482 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 138482 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
54585864 60645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430478 87253 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 87253 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
127031623 139149 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787131 139149 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
45279402 123589 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123589 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
16756187 93173 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 93173 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
20817800 70417 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70417 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
57404374 73148 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011535 73148 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
44417988 82421 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217403 82421 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
71227161 129187 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 129187 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691651 73464 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73464 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691737 73616 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73616 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11684745 16091 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 16091 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417943 82478 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217678 82478 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
23658492 178977 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470633 178977 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
44405430 71949 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71949 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
10083869 65574 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
20817864 76060 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 76060 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
45484974 197289 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL568649 197289 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
44394883 126364 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 126364 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
54579971 60636 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760238 60636 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46835797 59751 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1725011 59751 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
11632909 133441 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 133441 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10377914 123174 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 123174 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
90666256 109366 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 109366 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
21062999 64618 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64618 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
46172937 59113 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
CHEMBL1697929 59113 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
11975436 79093 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 79093 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
3202885 40682 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
CHEMBL1484343 40682 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
11995139 82823 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL218031 82823 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562500 186735 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186735 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
44438747 93374 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 93374 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
54584857 60595 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760084 60595 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
46835810 59125 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1698337 59125 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
53318593 56710 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56710 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11605775 16041 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 16041 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405570 71992 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71992 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11994277 81640 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL216356 81640 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
15987265 196887 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 196887 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44425834 151416 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 151416 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417957 141905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL386880 141905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416777 80566 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214908 80566 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
44416872 80591 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215008 80591 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416838 80843 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL215256 80843 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417146 141433 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL384132 141433 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416955 141453 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL384233 141453 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416935 141664 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385410 141664 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417066 141952 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387217 141952 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416302 80048 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212958 80048 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416231 168990 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL439146 168990 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11201645 71871 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71871 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11995441 141961 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
CHEMBL387266 141961 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
57396294 68088 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 68088 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 68084 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 68084 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
1314 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
9865843 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
CHEMBL178707 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
11995243 82552 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217812 82552 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
11654412 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
11994661 82423 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL217410 82423 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
21940083 64718 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64718 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
127031355 139168 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787345 139168 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
23532180 68851 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922258 68851 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57403785 68862 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68862 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410876 76105 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 76105 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
45279868 123591 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123591 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
46172920 59254 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1703562 59254 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
45382322 59687 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
CHEMBL1722551 59687 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
11995645 141554 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384805 141554 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995647 141990 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL387420 141990 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562415 176965 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176965 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44394770 123840 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123840 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417971 141543 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL384734 141543 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11692293 93459 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93459 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417841 81590 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81590 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44405486 140512 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 140512 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405412 71874 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71874 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44405468 133432 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 133432 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
11974130 80362 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 80362 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394921 66240 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 66240 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
90666097 109330 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 109330 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666265 109376 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 109376 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430465 93299 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 93299 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
20817763 140583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410904 172457 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 172457 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394769 66915 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66915 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
54580458 60581 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760061 60581 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
22254581 66225 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 66225 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44396952 66728 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66728 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397262 67508 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67508 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44394705 125321 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 125321 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10262766 66979 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66979 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70685338 73480 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73480 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689595 73561 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73561 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11691995 16118 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 16118 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
44397425 66877 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66877 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
16756638 93229 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 93229 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
46172939 59844 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1728621 59844 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46835805 59849 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
CHEMBL1728794 59849 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
44438750 93413 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 93413 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414455 80272 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 80272 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
70685347 73509 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73509 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44410849 138297 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 138297 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44405651 71930 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71930 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
46172942 59145 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1698879 59145 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
70691739 73624 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73624 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405619 72504 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72504 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44397127 67083 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 67083 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
49866087 16243 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16243 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
70693796 73568 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73568 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16755870 144486 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 144486 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756402 92846 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92846 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
46172928 59708 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1723453 59708 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172932 59880 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
CHEMBL1729749 59880 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
70693794 73558 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73558 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
44414499 80327 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 80327 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
23027181 197208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568209 197208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44562563 174360 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 174360 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11452268 81573 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81573 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
23532172 68852 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922259 68852 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
44394859 66246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 66246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46846324 59410 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1710048 59410 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846320 59982 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
CHEMBL1733974 59982 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
11974346 141500 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 141500 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11612098 70284 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 70284 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44395076 66996 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66996 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
44414518 77909 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77909 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 80181 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 80181 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666266 109377 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 109377 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23120572 196063 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 196063 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
70683241 73503 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73503 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73511 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73511 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442064 154808 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154808 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
70683286 73555 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73555 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11975438 80232 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 80232 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
23027527 196792 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 196792 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57393332 68860 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68860 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68861 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68861 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
70687552 73621 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73621 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11993895 80382 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214468 80382 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
11305934 3849 3 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
1315 3849 3 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
CHEMBL2147477 3849 3 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
11993896 81103 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL215591 81103 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
56589628 68149 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 68149 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44416845 80545 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL214824 80545 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416814 80816 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL215234 80816 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
44416815 141474 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384346 141474 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
44417151 141555 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL384806 141555 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
44417145 141583 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL384988 141583 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416315 79834 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212137 79834 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416376 141427 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL384113 141427 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
23022536 76384 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76384 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
57523086 76391 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76391 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
23027402 197291 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568663 197291 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
22251624 64712 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64712 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57521366 76395 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76395 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44414570 78039 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 78039 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
11531010 133588 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133588 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
45485043 197205 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
CHEMBL568183 197205 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
49865738 16116 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 16116 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16755968 92492 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92492 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394650 65482 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65482 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
11974229 82483 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82483 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11778029 66209 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 66209 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
127031908 139172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787417 139172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11553648 73478 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73478 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
46850886 59918 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
CHEMBL1731173 59918 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
70691721 73556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417828 80681 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80681 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44410823 75554 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75554 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
44410821 77123 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 77123 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16755872 92496 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92496 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44405459 133156 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 133156 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
44417931 141594 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
CHEMBL385037 141594 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
22254632 124096 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 124096 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
11995240 81100 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
CHEMBL215580 81100 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
70695914 73557 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73557 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11603897 124328 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 124328 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394763 67052 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 67052 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
46835800 59347 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1707135 59347 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46835816 60049 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1736481 60049 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
49865790 16142 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 16142 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485038 197283 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568604 197283 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
54584905 60634 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760236 60634 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44405612 135479 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 135479 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
1091600 27831 15 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
CHEMBL1371138 27831 15 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
49865929 16196 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16196 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
21062990 64700 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64700 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11591644 16090 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 16090 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16756186 93172 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 93172 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
10389978 69614 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69614 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
887424 56169 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1582334 56169 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1626085 56169 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
90666263 109374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 109374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
10025899 77065 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 77065 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11512135 70308 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 70308 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11201867 98686 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98686 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
70691656 73508 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73508 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562564 189138 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 189138 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
54585374 60582 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760062 60582 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
16756184 92139 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 92139 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
46172936 59265 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
CHEMBL1703918 59265 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
44394958 66905 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66905 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
20817762 77325 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 77325 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
46835813 59959 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1732922 59959 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46835807 60004 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
CHEMBL1734822 60004 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
11994018 81021 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215374 81021 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11995445 82446 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL217535 82446 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
9887864 179083 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
CHEMBL471651 179083 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
52917998 60632 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60632 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23022422 74891 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74891 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10274635 68859 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68859 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
10360874 64934 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64934 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
44394698 66241 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 66241 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
1305 511 14 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 511 14 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 511 14 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
57392824 68083 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 68083 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11548234 71196 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 71196 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45485028 197166 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567950 197166 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
18436066 74894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74894 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11995443 80402 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214532 80402 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
16043291 79993 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79993 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
9910346 64732 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64732 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
44417022 80396 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214512 80396 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44417083 80910 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215298 80910 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
54580457 60579 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60579 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23120550 196606 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 196606 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
127033945 138953 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138953 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44394725 66151 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 66151 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44405482 71851 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71851 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
57395049 68843 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922250 68843 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46172917 59536 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
CHEMBL1716369 59536 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
11775505 141987 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141987 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
127031354 139105 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 139105 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44562600 173131 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 173131 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
49865679 16061 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 16061 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11419666 122553 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122553 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
16756752 142591 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142591 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
10137322 149408 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 149408 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44410838 77061 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 77061 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16756751 93310 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 93310 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
44397128 124102 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 124102 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
46172930 60033 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1735852 60033 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
11328029 76530 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76530 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
11634061 192353 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 192353 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
70693792 73548 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73548 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73550 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73550 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10388797 71759 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71759 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
46835804 59476 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1713871 59476 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
127033095 139071 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786352 139071 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
46835802 59419 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1710499 59419 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
49865869 16177 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 16177 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397026 127170 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 127170 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44417946 82452 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217557 82452 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
58062359 125875 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
CHEMBL3648385 125875 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
44438740 93937 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93937 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
46892785 125882 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
CHEMBL3648392 125882 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
44418005 82394 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217257 82394 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
11974345 80340 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 80340 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11259253 82545 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82545 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
90469437 121270 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 121270 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44394798 124385 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 124385 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
11995136 80912 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL215307 80912 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
49865708 16089 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 16089 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485061 198754 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 198754 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44442090 94160 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 94160 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
10067783 66200 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 66200 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
44414451 168939 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168939 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
18436083 74889 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74889 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994136 141938 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
CHEMBL387085 141938 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
18436055 74874 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74874 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
90666260 109370 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 109370 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
11662906 73479 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73479 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46172923 59385 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
CHEMBL1708907 59385 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
3114950 37769 32 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37769 32 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
44562403 189828 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189828 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
45485003 198374 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL576665 198374 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
11583835 73482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666253 109363 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 109363 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
44394607 124353 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 124353 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11569300 82482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
45382327 59250 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
CHEMBL1703414 59250 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
70687478 73501 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73501 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11619850 75776 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75776 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
23657037 94524 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94524 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693793 73554 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73554 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44592256 189375 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL512873 189375 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
11973916 141496 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 141496 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
54582014 60627 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760227 60627 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
46835792 59659 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
CHEMBL1721648 59659 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
2042108 47984 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
CHEMBL1549996 47984 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
58062337 125876 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
CHEMBL3648386 125876 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
45271839 196547 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 196547 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44442139 94458 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94458 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
49865680 16062 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 16062 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 16117 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 16117 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11649549 93938 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93938 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
70685396 73560 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73560 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11776033 67172 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 67172 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11995241 80561 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
CHEMBL214891 80561 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
1314 3727 21 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3727 21 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3727 21 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11190261 63243 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 63243 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
11592199 16119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 16119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
20817846 138696 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138696 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10456755 71098 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 71098 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395019 66237 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 66237 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
70681197 73562 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73562 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10344176 67185 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 67185 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
4033 1899 48 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
9826520 1899 48 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
CHEMBL214957 1899 48 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
44397194 66981 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66981 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44394638 123799 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123799 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
52917999 60644 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60644 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430458 142811 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142811 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
70696356 74842 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74842 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70685337 73473 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73473 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16244 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16244 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
11281523 81802 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81802 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
11153928 165780 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165780 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
23593464 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436075 74845 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74845 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57401509 68087 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 68087 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
23593464 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11995028 141438 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
CHEMBL384147 141438 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
45485077 197203 1 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL568162 197203 1 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
11547939 161283 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
CHEMBL412135 161283 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
44414483 79733 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79733 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45267577 195968 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 195968 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11165058 154632 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154632 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
11633862 179167 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 179167 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10083869 65574 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
10083869 65574 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65574 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397476 67426 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67426 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
44417981 165981 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425269 165981 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
54582961 60640 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60640 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
21939767 64698 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64698 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70689519 73457 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73457 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689596 73563 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73563 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394596 66205 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 66205 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11554989 179063 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 179063 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
10070680 72109 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 72109 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
56597990 139185 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787582 139185 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
11526824 16120 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 16120 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405557 132751 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132751 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
1017287 56022 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1568072 56022 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1624689 56022 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
45268470 196295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 196295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
45268465 196561 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 196561 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
54585861 60628 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760228 60628 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2729502 81052 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 81052 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
46172925 59470 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
CHEMBL1713683 59470 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
44417972 141593 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385036 141593 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
90666267 109378 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 109378 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
49865927 16194 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16194 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
44417952 141742 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385876 141742 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973800 81572 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81572 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442071 154614 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154614 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
49865871 16179 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 16179 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49866086 16242 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16242 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11634230 70174 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 70174 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
46835794 59538 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1716381 59538 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
1746683 31299 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
CHEMBL1401638 31299 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
11520239 3632 11 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
1313 3632 11 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
CHEMBL185271 3632 11 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
11236807 81566 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
16037921 140173 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380371 140173 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945130 17049 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254563 17049 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44412852 138403 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377321 138403 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943873 17034 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254400 17034 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52945087 17035 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254401 17035 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
11191034 79864 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212256 79864 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942885 17041 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254481 17041 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
10230947 72582 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199274 72582 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413473 97272 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL268938 97272 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413297 138412 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377372 138412 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44413474 167465 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL429895 167465 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52948758 17040 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254480 17040 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945129 17048 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254562 17048 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52950112 17075 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254797 17075 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417918 81547 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216103 81547 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
44417928 96417 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL261964 96417 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
23626228 89325 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL236889 89325 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417919 80873 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215278 80873 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
44417905 82472 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217637 82472 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52949912 17028 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254328 17028 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44424263 85787 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229406 85787 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
44434153 145242 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL391275 145242 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
44417993 81765 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216406 81765 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
10303281 133566 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL371099 133566 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44417922 82553 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL217820 82553 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
20609028 138895 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378269 138895 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11592317 139525 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL379521 139525 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44418004 168821 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL437728 168821 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
11236807 81566 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11236807 81566 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
52947407 17009 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254148 17009 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11634329 142300 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL388524 142300 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
11634329 142300 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
CHEMBL388524 142300 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
20608975 77763 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209089 77763 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434151 89614 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL237531 89614 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
10166088 72410 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
CHEMBL198724 72410 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
44413138 138894 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378261 138894 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52947140 17117 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255054 17117 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413326 79863 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212254 79863 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946021 16953 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253628 16953 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11236807 81566 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11156790 77932 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209510 77932 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
16659197 97082 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL267320 97082 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10311798 79989 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212750 79989 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
10128764 78308 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210857 78308 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417901 80315 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL214178 80315 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
44417895 165855 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL424895 165855 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44424260 85778 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229348 85778 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
44417967 82297 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217196 82297 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
10143980 72481 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198945 72481 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943978 16938 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253196 16938 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52947331 16981 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253875 16981 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52942540 17011 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254150 17011 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943913 17047 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254561 17047 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52949472 17064 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254714 17064 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945155 54976 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254636 54976 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615721 54976 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
44413475 78008 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL209754 78008 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
11497179 79768 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211820 79768 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417950 172754 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL450942 172754 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44413470 78392 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211069 78392 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417923 82581 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL217875 82581 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44405437 71948 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197280 71948 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405417 72554 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199179 72554 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405461 71856 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197005 71856 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
52941493 54978 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254564 54978 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615759 54978 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
10196608 77311 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208275 77311 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10312244 139513 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL379489 139513 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
11691468 169344 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL441886 169344 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
16659239 141883 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL386717 141883 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
15982955 93648 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL246794 93648 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10239929 78102 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210255 78102 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11692382 169374 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL442084 169374 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
44434148 89517 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237318 89517 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
52944859 16974 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253795 16974 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44434155 169395 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL442244 169395 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
44413428 78617 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
CHEMBL211232 78617 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
10196214 78131 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210344 78131 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405439 72488 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198969 72488 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129058 138665 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL377738 138665 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44417916 82137 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216741 82137 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10239448 78169 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210436 78169 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52944540 17065 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254715 17065 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44417913 81589 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216314 81589 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
10143421 72349 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198483 72349 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44434149 148654 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL393959 148654 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
20608974 79882 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212330 79882 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
17989329 81081 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL215508 81081 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
20608989 78202 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210532 78202 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44412960 79969 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL212671 79969 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
10174984 78109 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210274 78109 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945048 17026 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254326 17026 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948916 17029 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254329 17029 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
10209344 123254 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL361392 123254 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10165503 125953 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL364871 125953 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946184 17017 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254240 17017 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52942685 17039 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254479 17039 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946082 16982 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253876 16982 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52941054 17118 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255055 17118 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11317465 138201 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL376976 138201 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413472 138691 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377864 138691 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417926 81123 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215660 81123 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
52941272 16993 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253963 16993 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52947141 17120 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1255057 17120 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
23573799 72399 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198689 72399 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
10196316 78201 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210531 78201 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943353 17063 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254713 17063 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
70681299 73962 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
CHEMBL2021397 73962 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
10218547 77735 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208970 77735 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44434143 89324 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL236888 89324 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
11657090 79730 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL211615 79730 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417909 157713 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL408198 157713 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
11628547 139271 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL379060 139271 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417969 81577 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216242 81577 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44405435 72487 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198968 72487 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10218604 138866 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378180 138866 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417953 81585 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216280 81585 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52943912 17046 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254560 17046 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44417904 80377 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL214432 80377 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
10174522 139681 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379797 139681 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417900 81537 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216050 81537 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44417933 141510 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL384546 141510 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
20608996 77755 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209059 77755 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
20608991 77753 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209050 77753 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52946062 16975 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253796 16975 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412837 77275 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL208081 77275 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
11433168 138693 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138693 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413309 138908 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378310 138908 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949812 16999 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254055 16999 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10165656 71818 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196864 71818 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943485 17119 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255056 17119 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10129026 78304 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210818 78304 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405399 135997 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373165 135997 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943712 17001 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254057 17001 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44592215 188831 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
CHEMBL506480 188831 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
10196098 78023 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209828 78023 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10289494 78276 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210715 78276 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196460 79838 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212159 79838 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44592169 178832 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
CHEMBL469343 178832 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
44592214 189356 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL512657 189356 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
44417887 141484 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384400 141484 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52948636 17021 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254244 17021 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11570040 77769 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209109 77769 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11698592 78057 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209993 78057 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11613696 135255 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL372551 135255 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413283 79737 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211672 79737 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
20609018 140156 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380275 140156 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52948553 16983 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253877 16983 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945088 17037 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254403 17037 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
44417924 141406 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL384030 141406 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
44417892 80236 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL213771 80236 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
44405501 71879 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197065 71879 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
44413299 77370 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208573 77370 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413312 79647 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211511 79647 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949479 17077 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254799 17077 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44424266 85788 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229407 85788 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
11664086 77713 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208931 77713 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417889 141405 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384000 141405 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
10312086 79851 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212210 79851 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52946137 16998 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254054 16998 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52940981 17088 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254885 17088 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417960 81796 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL216429 81796 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
10186370 71809 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196819 71809 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
11642443 77627 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208827 77627 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
52947314 16972 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253793 16972 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
11318709 139669 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379789 139669 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434156 145528 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL391496 145528 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
10152879 78857 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211285 78857 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52945863 17103 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254972 17103 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947542 17042 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254482 17042 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947539 17033 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254399 17033 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11635274 138688 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377843 138688 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942539 17008 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254147 17008 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
20608977 139252 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378972 139252 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11628136 77775 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209123 77775 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
20608976 78130 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210343 78130 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434144 167309 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL429393 167309 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
11527169 77379 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL208635 77379 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
44434146 89442 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237099 89442 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
20608992 78348 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211005 78348 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44413471 79615 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211492 79615 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44412682 78453 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211166 78453 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944920 17000 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254056 17000 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413345 141494 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
CHEMBL384449 141494 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
44417927 81086 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215526 81086 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52943689 16991 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
CHEMBL1253961 16991 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
52944577 17089 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254886 17089 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405421 72001 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197429 72001 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405418 135784 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373036 135784 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44412686 79025 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211311 79025 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196742 161721 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL413578 161721 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417963 166011 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL425445 166011 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52942547 17020 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254243 17020 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
52943420 17104 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254973 17104 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52948635 17018 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254241 17018 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946259 17027 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254327 17027 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44412624 78385 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211058 78385 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10129036 79824 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212093 79824 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11562056 79791 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211956 79791 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417893 80583 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL214983 80583 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
10152726 138729 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
CHEMBL378009 138729 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
44417912 82275 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217140 82275 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
11433168 138693 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138693 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947267 16954 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253629 16954 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948531 16973 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253794 16973 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44424270 85797 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL229463 85797 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
52943690 16992 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253962 16992 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
24963343 73149 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 73149 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
10239505 77930 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209504 77930 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44434154 89920 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL237959 89920 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
11512221 89823 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237748 89823 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
52947610 17054 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254634 17054 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10280331 141316 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL383390 141316 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
20608969 78183 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210481 78183 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44417920 80854 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215266 80854 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417987 82412 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217351 82412 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
20609011 138715 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377976 138715 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413480 79941 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL212573 79941 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
11635715 77443 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208688 77443 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
10239639 78161 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210408 78161 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52947054 17090 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254887 17090 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10281308 72366 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198562 72366 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413382 77767 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209103 77767 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11270012 82148 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216821 82148 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
52949955 17032 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254398 17032 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945806 17076 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254798 17076 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405436 71947 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197279 71947 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
11656916 138892 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL378242 138892 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417954 97260 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL268848 97260 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
44434152 89615 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237532 89615 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417898 82575 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL217860 82575 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
44405444 135198 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372116 135198 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129135 78046 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209935 78046 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
16106513 178882 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL469789 178882 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10218194 78419 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211139 78419 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413271 138393 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377270 138393 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
16659061 82576 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217861 82576 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
10239930 79639 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211504 79639 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52949693 16955 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253630 16955 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
20608981 79865 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212265 79865 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947408 17010 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254149 17010 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52941518 17055 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254635 17055 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943587 16956 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253631 16956 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10188732 135399 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372803 135399 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
44417934 82465 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217605 82465 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52949956 17036 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254402 17036 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
11497180 165765 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL424697 165765 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417929 81938 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216486 81938 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44417985 81564 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216187 81564 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
11752339 69399 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL193260 69399 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
10196576 139257 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL378994 139257 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52948951 17019 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254242 17019 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
52949768 16984 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253878 16984 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412683 79170 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211335 79170 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944948 17007 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254146 17007 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
44417891 80352 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214323 80352 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417908 82163 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216959 82163 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44413259 139690 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
CHEMBL379802 139690 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
44434145 89440 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237098 89440 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
10152629 141533 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL384676 141533 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413398 77947 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209590 77947 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11520239 3632 11 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3632 11 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3632 11 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
54579974 3240 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7756 3240 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
CHEMBL1760248 3240 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7735 536 11 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
9927967 536 11 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
CHEMBL400679 536 11 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
1305 511 14 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
9934033 511 14 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
CHEMBL182150 511 14 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1314 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
9865843 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
CHEMBL178707 3727 21 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
24890862 1108 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
7755 1108 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
57523087 1158 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
7754 1158 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
CHEMBL2059513 1158 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
57521365 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
57521365 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
8587 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
8587 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
CHEMBL2059420 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
CHEMBL2059420 2615 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
56835134 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
7753 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
CHEMBL1934835 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
4033 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
9826520 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
CHEMBL214957 1899 48 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
1292 1059 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1290 258 0 None 15 2 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1307 528 0 None -1 2 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
11305934 3849 3 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1315 3849 3 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
CHEMBL2147477 3849 3 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1300 3088 0 None - 1 Human 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
11539096 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1303 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
CHEMBL214021 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1297 3103 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1297 3103 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159839
1297 3103 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
11994411 1004 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
1306 1004 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
CHEMBL214523 1004 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
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

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 DOI
44219756 178692 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
CHEMBL468099 178692 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
44219756 178692 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
CHEMBL468099 178692 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
44442095 94302 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 94302 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11648912 80351 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 80351 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
45487671 197279 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568571 197279 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44574008 189225 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL511542 189225 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
9915039 60823 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL176219 60823 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
45487668 196997 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566880 196997 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
45271549 195573 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 195573 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
24762415 198747 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL582978 198747 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44417966 161518 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 161518 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 169019 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 169019 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10118862 60802 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL176159 60802 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
45487674 198724 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL582792 198724 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
10258364 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538424 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538425 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
18436066 74894 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74894 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10258364 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10360874 64934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10230490 63179 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL178997 63179 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
10345845 178473 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 178473 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
22018957 82442 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82442 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11561126 68861 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68861 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68861 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL1922270 68861 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
18436114 74892 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74892 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
9932896 74527 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74527 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
9932896 74527 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74527 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10004545 74952 7 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
46933538 16216 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16216 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417832 141752 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141752 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10258364 194784 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10459635 196695 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL564788 196695 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
18436055 74874 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74874 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
70696356 74842 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74842 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417948 141749 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141749 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22348140 168723 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168723 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
45273335 195830 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL558305 195830 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
10114686 60570 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175993 60570 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
10067783 66200 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 66200 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10000146 64647 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64647 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11201645 71871 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71871 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57393332 68860 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68860 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410849 138297 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 138297 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
90666096 109329 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 109329 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44407944 166002 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 166002 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70688018 74843 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74843 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11705240 132813 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132813 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
18436094 74885 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74885 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
21108114 68074 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 68074 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10226765 123136 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL361215 123136 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394650 65482 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65482 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394800 122356 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 122356 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394609 123885 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123885 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
10248906 123653 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123653 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
16721015 80421 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80421 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11583193 141809 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL386281 141809 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018944 82208 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 82208 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
22018964 141670 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141670 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
56835134 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
7753 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
CHEMBL1934835 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
25058425 60773 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761103 60773 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114286 60789 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761119 60789 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
57890345 122405 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
CHEMBL3600810 122405 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
60130264 122406 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
CHEMBL3600811 122406 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
10413283 187468 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL494016 187468 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
18436117 74893 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74893 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
44557554 196411 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 196411 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
9932896 74527 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74527 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10481477 195685 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL556697 195685 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
44417875 80794 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80794 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22348022 77351 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 77351 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
57521365 2615 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2615 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2615 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
10231341 63346 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL179437 63346 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
10113523 129816 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL367532 129816 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394769 66915 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66915 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10150552 81593 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81593 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417959 81795 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81795 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141817 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141817 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
57392823 68081 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 68081 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
22348155 76585 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76585 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44555375 196802 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL565614 196802 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436038 76374 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76374 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417845 141886 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141886 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11627530 75910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487660 199026 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL585856 199026 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10345845 178473 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 178473 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
18436085 74888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522703 76376 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76376 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417846 82099 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 82099 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939937 64717 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64717 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11775399 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
CHEMBL179501 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
45487647 196921 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566257 196921 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436083 74889 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74889 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436082 74890 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74890 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56708 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56708 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11775399 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
CHEMBL179501 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
11713027 81174 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 81174 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
11775399 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63360 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11775399 63360 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL179501 63360 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44417998 82395 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 82395 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150954 141547 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141547 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11548234 71196 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 71196 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10027853 71862 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71862 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57523087 1158 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1158 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1158 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
57523086 76391 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76391 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
11496313 72312 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 72312 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21939898 64726 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64726 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
18435902 76375 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76375 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11613073 75930 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75930 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44573931 187452 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL493962 187452 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
23022536 76384 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76384 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
9932896 74527 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74527 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
22251624 64712 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64712 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23022422 74891 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74891 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
18435902 76375 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76375 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10183297 93312 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
CHEMBL245231 93312 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
44402563 71672 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196388 71672 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
10005009 166376 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 166376 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21940083 64718 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64718 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64732 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64732 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10345121 187453 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
CHEMBL493967 187453 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
9910346 64732 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64732 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522468 76394 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76394 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
57521365 2615 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2615 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2615 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
71730392 131292 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686821 131292 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730393 131293 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686822 131293 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730531 131300 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686829 131300 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44394763 67052 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 67052 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
44394683 67208 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 67208 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394591 122658 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122658 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123631 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123631 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394866 124349 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 124349 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11647458 81998 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216524 81998 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417925 81464 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81464 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141560 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141560 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
25115854 60771 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761101 60771 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70691736 73601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57845728 122439 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600971 122439 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
122184694 122489 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601035 122489 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184706 122502 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601047 122502 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89798657 122534 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601303 122534 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
59835853 122362 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600392 122362 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
60130301 122408 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600813 122408 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
59835871 122472 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601014 122472 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
9866552 80501 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
CHEMBL2147476 80501 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
11646818 166224 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL426666 166224 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817846 138696 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138696 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44407967 74492 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74492 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271134 195126 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550068 195126 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
11166395 94276 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250327 94276 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666095 109328 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 109328 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70693734 73477 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73477 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865927 16194 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16194 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
16072132 80427 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80427 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
10344176 67185 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL187756 67185 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44397202 67224 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 67224 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44390730 64317 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181099 64317 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403548 70392 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70392 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403523 70419 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70419 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403498 71078 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 71078 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403506 71134 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 71134 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
10025637 65584 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL183215 65584 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
44413474 167465 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL429895 167465 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
12020151 195188 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550545 195188 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44405431 71951 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71951 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
44394644 66136 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 66136 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 131452 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 131452 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11562129 71077 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 71077 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
60169181 87763 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337728 87763 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
54582961 60640 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60640 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
89691143 139315 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 139315 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
21108099 68157 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914860 68157 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18436118 74881 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
CHEMBL2031723 74881 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
23022589 74887 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031729 74887 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11633862 179167 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 179167 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10050565 75705 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75705 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403527 127175 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 127175 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403538 136111 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 136111 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44418001 141704 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385639 141704 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417822 80573 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214936 80573 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71717085 87782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337747 87782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71717701 87796 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337761 87796 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25115619 60767 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761097 60767 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
21939900 64699 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818780 64699 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
90666251 109361 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 109361 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70693737 73505 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73505 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
45269335 196463 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 196463 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44562522 194546 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL529450 194546 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71716478 87783 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337748 87783 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397303 66841 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186160 66841 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
155528494 171349 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
CHEMBL4461504 171349 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
11776033 67172 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 67172 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70693810 73625 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73625 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44407966 75895 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204912 75895 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
11605260 70636 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70636 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
44402535 166062 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL425744 166062 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
44442058 94357 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250728 94357 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49866089 16245 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16245 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44403499 71117 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 71117 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
70693792 73548 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73548 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10399674 66120 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184001 66120 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11569340 71650 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71650 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11677806 186009 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL487040 186009 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70685396 73560 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73560 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
71226697 129180 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 129180 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730920 131227 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686755 131227 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759545 131244 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686772 131244 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730390 131289 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686818 131289 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759570 131291 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686820 131291 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417897 141425 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL384111 141425 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
70689612 73604 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73604 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
71816518 138284 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 138284 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
21062999 64618 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64618 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
122184562 122411 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600816 122411 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978378 122468 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601010 122468 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89702226 139313 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 139313 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57391028 68085 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 68085 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57401510 68090 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 68090 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
56589628 68149 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 68149 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11328029 76530 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76530 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
45271908 195534 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL554287 195534 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
23120582 196286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562074 196286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
45273802 194833 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
CHEMBL539475 194833 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
45487385 196842 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
CHEMBL565834 196842 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
45487356 197832 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572300 197832 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666094 109327 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 109327 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666262 109373 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 109373 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
11605775 16041 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 16041 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
127031338 139072 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 139072 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
49801837 139010 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 139010 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
123471111 139138 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 139138 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 139170 27 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 139170 27 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11563017 81062 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 81062 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44405481 71850 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71850 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
89690237 138224 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 138224 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
54580457 60579 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60579 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
117816753 139337 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 139337 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
89691057 139471 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 139471 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436095 74886 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031728 74886 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11592199 16119 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 16119 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865868 16176 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 16176 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397009 66759 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL185843 66759 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44397310 67312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188401 67312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403471 141343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
CHEMBL383567 141343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
23567394 60874 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176230 60874 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
10420382 166305 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL427153 166305 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417866 80549 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214843 80549 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417827 81102 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215586 81102 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417996 166103 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL425979 166103 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135474 91528 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403867 91528 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16192241 48736 3 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
CHEMBL1558309 48736 3 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
44394966 122961 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL360811 122961 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
11605260 70636 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70636 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
45272006 195238 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550943 195238 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44562501 185998 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
CHEMBL487022 185998 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
70695930 73618 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73618 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45268637 196177 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL561344 196177 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
49865929 16196 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16196 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562562 174358 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455143 174358 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11518159 135261 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372570 135261 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
3410248 71097 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL195350 71097 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
11973916 141496 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 141496 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
22254632 124096 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 124096 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
91759549 131253 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686781 131253 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683286 73555 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73555 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
70689520 73466 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73466 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683241 73503 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73503 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
46899582 16952 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253627 16952 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45267849 196132 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL561092 196132 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44442059 94358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250729 94358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759566 131283 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686812 131283 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730391 131290 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686819 131290 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417921 81125 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 81125 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
10310161 97081 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL267319 97081 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018896 141694 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141694 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57392549 69644 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934837 69644 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89689924 138332 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 138332 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
52917999 60644 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60644 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
59835799 122477 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601019 122477 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
23593474 64703 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64703 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21062998 64715 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64715 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
21939915 64716 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64716 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
21940008 64725 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64725 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57399741 68089 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 68089 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11419337 166161 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL426292 166161 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
44410876 76105 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 76105 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410944 77052 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 77052 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10025899 77065 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 77065 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11973800 81572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44143492 193482 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526647 193482 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522948 76388 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76388 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
53322554 56706 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642473 56706 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53320117 56722 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56722 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
90666266 109377 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 109377 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23022509 76381 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76381 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
18436119 76382 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76382 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57521366 76395 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76395 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407629 168654 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168654 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487653 199007 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 199007 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11419337 166161 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL426292 166161 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10041636 123195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 123195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417838 81597 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81597 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
60168913 87776 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337741 87776 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57397816 69618 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934811 69618 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690573 138312 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 138312 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89690573 138312 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 138312 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89691019 139393 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 139393 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267724 196128 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL561083 196128 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
11561155 190908 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518515 190908 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
46902024 17101 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254968 17101 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44397560 67730 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
CHEMBL190775 67730 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
57396293 68077 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914626 68077 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390748 64352 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181251 64352 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417994 81766 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL216407 81766 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
70691721 73556 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73556 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44403501 69650 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69650 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44393379 65298 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL182886 65298 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
45270302 195420 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL552224 195420 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
44573964 178654 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
CHEMBL467668 178654 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
44407951 75374 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203804 75374 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
44562523 186761 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488887 186761 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44417902 81072 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL215457 81072 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
155527803 171270 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4460423 171270 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
71226697 129180 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 129180 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730130 131271 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686800 131271 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730132 131273 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686802 131273 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730395 131297 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686826 131297 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730529 131298 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686827 131298 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730530 131299 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686828 131299 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417894 80584 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80584 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417973 141475 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 141475 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417823 165772 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165772 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417956 96651 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96651 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184701 122497 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601042 122497 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
122184702 122498 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601043 122498 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
52917998 60632 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60632 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89798658 122526 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601295 122526 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
56680348 64721 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64721 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89691096 139477 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 139477 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11973799 82462 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82462 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
44407860 75421 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75421 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271095 195229 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL550876 195229 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
23022499 74846 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
CHEMBL2031577 74846 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
44442120 94250 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250123 94250 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11505089 194807 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 194807 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866035 16230 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16230 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522950 76390 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76390 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
24952418 91517 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91517 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
56598130 139150 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 139150 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407875 75062 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 75062 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44413326 79863 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL212254 79863 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
44394946 65275 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL182847 65275 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
44417867 141513 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 141513 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71718318 87790 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337755 87790 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
89690622 138336 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 138336 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798780 139391 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 139391 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798680 139377 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 139377 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798688 139468 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 139468 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
45268527 196462 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL563147 196462 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
155569743 86059 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL2308118 86059 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
23593471 64706 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818787 64706 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44394861 66213 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184454 66213 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44413138 138894 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL378261 138894 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10377914 123174 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 123174 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11974126 141953 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL387219 141953 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
91759553 131256 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686784 131256 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
11386451 71872 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197054 71872 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
44143500 192952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL522242 192952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
57402226 69404 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1933085 69404 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
10332650 66194 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 66194 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254571 66969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
45270297 195353 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551826 195353 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
90666255 109365 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 109365 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
44442098 94048 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248881 94048 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
86695567 131231 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686759 131231 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
86695568 131232 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686760 131232 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759567 131286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686815 131286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
57392546 69623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934816 69623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397817 69624 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934817 69624 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
52918016 60646 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60646 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
1314 3727 21 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3727 21 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3727 21 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
56666754 64714 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64714 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89702566 139328 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 139328 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44407870 75914 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75914 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
90666265 109376 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 109376 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127030368 138977 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138977 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
56597851 139060 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 139060 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 80341 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 80341 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
16659197 97082 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL267320 97082 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
44395019 66237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 66237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44395076 66996 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66996 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
89691440 138167 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 138167 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21062991 64701 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64701 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56673714 64720 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64720 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
117798675 139360 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 139360 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89690973 139364 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 139364 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691284 139422 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 139422 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273638 195742 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557317 195742 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
49865789 16140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223967 16140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11678370 136565 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136565 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11284878 64343 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181217 64343 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401626 71354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195810 71354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
44403539 166280 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427006 166280 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
45271246 195207 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550683 195207 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
57397818 69638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934830 69638 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
70681114 73459 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73459 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45271647 195182 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550513 195182 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45273406 196401 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562788 196401 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
9804849 67456 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67456 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70687550 73614 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73614 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45271549 195573 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 195573 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
49866034 16229 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224304 16229 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11190261 63243 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 63243 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
44394983 66280 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 66280 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11974129 81114 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
CHEMBL215631 81114 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
44394825 66167 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184277 66167 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
60150483 73552 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73552 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10408758 122421 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600826 122421 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
71226268 129184 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
CHEMBL3670641 129184 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
71225855 129186 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
CHEMBL3670643 129186 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
91759571 131294 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686823 131294 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
10025637 65584 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65584 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
57399486 69625 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934818 69625 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
122184698 122493 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601039 122493 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
122184704 122500 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601045 122500 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89702233 138202 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 138202 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184565 122414 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600819 122414 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44438748 149497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 149497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
22348066 165830 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165830 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
10024175 188037 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497619 188037 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
7735 536 11 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
9927967 536 11 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
CHEMBL400679 536 11 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
11419776 94251 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250124 94251 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666264 109375 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 109375 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70691652 73472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685338 73480 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73480 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865928 16195 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16195 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
71227161 129187 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 129187 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597988 139153 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 139153 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 80341 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 80341 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
44408027 75067 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 75067 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
44390710 64589 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181632 64589 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
71227171 129194 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
CHEMBL3670650 129194 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
44417967 82297 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
CHEMBL217196 82297 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
44417895 165855 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL424895 165855 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
10434776 126382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 126382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405430 71949 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71949 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
70691722 73565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73565 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89690292 138188 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 138188 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025096 138227 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 138227 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
89691440 138167 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 138167 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127029759 139365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
CHEMBL3793053 139365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
53325163 56702 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642469 56702 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45270803 195079 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL549636 195079 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
90666257 109367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 109367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70695853 73469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553648 73478 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73478 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685347 73509 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73509 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11526824 16120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 16120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562461 188900 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL507549 188900 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
44390499 129657 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367355 129657 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11284878 70441 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194602 70441 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
11656044 141137 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 141137 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184673 122449 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600981 122449 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
45267746 196436 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL563005 196436 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
44438739 93936 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248295 93936 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
16742745 122485 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601031 122485 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
44397716 168314 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL434156 168314 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
11662564 133526 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 133526 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395012 66294 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184797 66294 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11974345 80340 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 80340 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
22266820 205045 25 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL77072 205045 25 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
71226964 129181 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 129181 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71730663 122548 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601376 122548 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759548 131252 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686780 131252 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732079 131270 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686799 131270 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759579 131309 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686837 131309 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
9804849 67456 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67456 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 70322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 70322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44403742 71719 6 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL196573 71719 6 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
10388797 71759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25114068 60786 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761116 60786 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685407 73600 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73600 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
9980157 122440 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600972 122440 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730663 122548 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601376 122548 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
89691096 139477 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 139477 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11653882 141305 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL383359 141305 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817763 140583 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140583 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
9804849 67456 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67456 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
53318595 56724 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642493 56724 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44442134 94192 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249716 94192 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
56597542 138951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627530 75910 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75910 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407836 75266 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 75266 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11562138 70518 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70518 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
60168915 87777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337742 87777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690973 139364 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 139364 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45270157 195069 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL549583 195069 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
9895868 12899 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL1188966 12899 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL537846 12899 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10231050 64334 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181184 64334 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9895868 69582 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69582 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403492 70629 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
CHEMBL195006 70629 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
44403490 71656 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196362 71656 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
18436043 76378 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059412 76378 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44397605 67509 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189508 67509 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44408093 140898 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382126 140898 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
49865870 16178 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224081 16178 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44394854 66914 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186547 66914 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11189610 165777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44438741 93824 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93824 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417937 141558 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL384844 141558 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
44388409 166239 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 166239 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
46902025 17116 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1255050 17116 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
70681198 73573 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73573 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562524 186762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
CHEMBL488890 186762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
11973802 82127 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL216680 82127 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
71731806 122527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3601296 122527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732078 122531 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601300 122531 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71731045 131275 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686804 131275 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730788 131323 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686851 131323 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
44417886 141698 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141698 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
122184670 122441 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600973 122441 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
89702233 138202 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 138202 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71731806 122527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601296 122527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
71732078 122531 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601300 122531 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
21062990 64700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
9844702 64707 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64707 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
59835874 122479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601020 122479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89691044 139479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 139479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89690957 139325 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 139325 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57399741 68089 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 68089 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11692293 93459 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93459 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
23120580 196041 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL560334 196041 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407667 74406 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74406 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
45267735 196317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL562285 196317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
45271673 195374 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL551924 195374 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
44250210 195947 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
CHEMBL559535 195947 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
70685337 73473 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73473 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57401248 69620 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934813 69620 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
89702355 138200 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 138200 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798692 139346 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 139346 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
18436109 76379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059413 76379 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417017 80380 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 80380 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11620005 81456 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81456 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397309 67528 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189602 67528 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44390707 129668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367359 129668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11973802 82127 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
CHEMBL216680 82127 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
44417825 141650 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385361 141650 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
70681197 73562 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73562 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417991 82433 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217459 82433 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
90666252 109362 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 109362 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45271663 196571 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL563884 196571 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
155516078 170050 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4442916 170050 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
10262766 66979 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66979 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11568782 71899 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71899 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
46899578 16980 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253872 16980 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11974030 155276 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 155276 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11211551 167263 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL429301 167263 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
57399487 69637 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934829 69637 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
71226697 129180 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 129180 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71225842 129185 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
CHEMBL3670642 129185 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
71730131 131272 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686801 131272 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730264 131282 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686811 131282 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730265 131284 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686813 131284 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759569 131288 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686817 131288 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
71730534 131311 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686839 131311 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759586 131320 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686848 131320 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730789 131324 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686852 131324 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71714121 122549 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122549 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
10173787 82438 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82438 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141768 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
89691044 139479 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 139479 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436126 74878 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031720 74878 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
53318592 56703 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
CHEMBL1642470 56703 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
53326457 56721 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642490 56721 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
10050565 75705 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75705 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139559 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139559 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408108 139814 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139814 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417979 82146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 82146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417940 81694 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81694 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11539632 70561 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70561 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
71718910 87771 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337736 87771 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89702355 138200 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 138200 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53324269 56720 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642489 56720 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687471 73468 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73468 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11691995 16118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 16118 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
45270416 196653 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL564409 196653 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44403733 72444 4 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
CHEMBL198823 72444 4 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
70693795 73559 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73559 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45178545 173217 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
CHEMBL4522986 173217 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
44394987 66229 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184534 66229 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
90666259 109369 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 109369 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
44402420 141372 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL383798 141372 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
122184703 122499 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601044 122499 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
137655884 158758 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158758 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
11974035 82623 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
CHEMBL217925 82623 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
137655884 158758 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158758 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
71226964 129181 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 129181 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71225843 129182 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670639 129182 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
71731803 131226 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686754 131226 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730919 131240 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686768 131240 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730266 131285 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686814 131285 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759568 131287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
CHEMBL3686816 131287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
71731048 131317 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686845 131317 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730662 131318 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686846 131318 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL4115910 212951 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL None None None None nan
44417939 82382 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL217233 82382 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
9804849 67456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114723 60793 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761124 60793 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
89690396 138252 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 138252 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
23593468 64704 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64704 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89702226 139313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 139313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57401507 68078 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914627 68078 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57392835 68151 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914854 68151 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44143493 188046 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497647 188046 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45273801 195705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL556927 195705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44573823 193234 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL523697 193234 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
70687477 73500 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73500 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522949 76389 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76389 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
9804849 67456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67456 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11612098 70284 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 70284 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11518384 165907 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL425013 165907 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
44417858 80381 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214450 80381 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71719523 87769 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337734 87769 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
21940052 64711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
17848895 68041 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914463 68041 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44403535 71427 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196004 71427 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44395007 124074 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL363264 124074 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
44401591 68897 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL192266 68897 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10377822 126824 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126824 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11837128 72130 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 72130 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
60168916 87778 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337743 87778 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44407836 75266 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 75266 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394999 66660 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL185348 66660 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11440885 82471 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217626 82471 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
44403533 71456 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71456 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44397329 67118 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187447 67118 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
45267709 195971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
CHEMBL559691 195971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
44394958 66905 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66905 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403486 71510 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL196273 71510 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
11453830 63406 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
CHEMBL179606 63406 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
10466406 66348 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185095 66348 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44394891 65215 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 65215 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394726 66159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 66159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
22018856 80607 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80607 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
22018999 81119 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 81119 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417947 141511 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 141511 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22018945 141723 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141723 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417845 141886 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141886 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25115618 60768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761098 60768 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
9866745 122395 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600801 122395 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11743571 122397 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600803 122397 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184557 122398 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600804 122398 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
60130278 122401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600807 122401 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11592099 93502 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93502 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
11562138 70518 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
CHEMBL194697 70518 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
10070016 71463 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL196208 71463 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
9983233 76001 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 76001 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11683903 82429 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82429 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
11201867 98686 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98686 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
11583049 141948 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141948 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
23120572 196063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 196063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407629 168654 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168654 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436038 76374 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76374 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
57522947 76387 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76387 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11556070 195490 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
CHEMBL553196 195490 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
11628328 195539 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 195539 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
46933537 16063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 16063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522703 76376 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76376 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11583747 81495 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81495 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
11677277 141779 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141779 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
11598355 141803 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141803 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44390726 122404 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL360081 122404 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
11562138 70518 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70518 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
10047339 70405 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70405 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417962 82086 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 82086 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71932 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71932 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44573822 187465 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL494009 187465 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
44573821 192733 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL522037 192733 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
10224210 63311 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL179353 63311 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
11353174 80597 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215030 80597 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
44394798 124385 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 124385 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
21939950 64727 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64727 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939937 64717 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64717 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
45267576 196632 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 196632 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18436115 74873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031715 74873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
44417843 81961 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81961 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11511219 66135 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 66135 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 70322 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 70322 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11655872 71717 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71717 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
11511219 66135 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 66135 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139559 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139559 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939898 64726 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64726 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44408109 75543 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75543 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522946 76386 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76386 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57523087 1158 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1158 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1158 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
44402677 71733 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196599 71733 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
21940083 64718 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64718 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
23120550 196606 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 196606 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
57522816 76383 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76383 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
10273126 61146 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176548 61146 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
45487640 197244 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568361 197244 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44469273 197558 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 197558 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
44394770 123840 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123840 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11583744 71724 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71724 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
22251624 64712 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64712 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
9887476 193423 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526083 193423 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
10391177 189254 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
CHEMBL511747 189254 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
10159452 74844 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74844 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57523086 76391 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76391 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
10391177 189254 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL511747 189254 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
10310316 81120 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 81120 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939902 64719 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64719 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
18436075 74845 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74845 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417877 81137 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 81137 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10073934 187490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
CHEMBL494155 187490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
71226400 129183 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670640 129183 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
44413472 138691 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377864 138691 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
71731671 131225 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686753 131225 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730917 131237 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3686765 131237 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
71730134 131276 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686805 131276 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730787 131322 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686850 131322 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730792 131329 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686857 131329 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44394922 66141 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 66141 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394959 67210 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 67210 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44417905 82472 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82472 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44405618 72015 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 72015 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
44405560 72448 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72448 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405646 96873 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96873 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405557 132751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405612 135479 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 135479 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
11653882 141305 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 141305 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
10083869 65574 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65574 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10083869 65574 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417888 80405 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 80405 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417857 141656 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141656 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11632484 70334 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 70334 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
60169095 87759 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337724 87759 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396018 69621 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934814 69621 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394271 69622 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934815 69622 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394272 69628 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934820 69628 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401249 69629 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934821 69629 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57402992 69630 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934822 69630 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691725 73577 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73577 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184692 122486 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601032 122486 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
16742747 122488 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601034 122488 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89691439 138248 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 138248 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
10386162 122422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600827 122422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388352 122474 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601016 122474 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
21062999 64618 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64618 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
57398087 68075 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914624 68075 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
21108117 68155 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914858 68155 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
44438740 93937 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93937 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44442153 94047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 94047 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44562545 189103 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 189103 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11583835 73482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522948 76388 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76388 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
44455414 97418 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
CHEMBL269939 97418 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
44397194 66981 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66981 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44407710 73940 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73940 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
58646147 79085 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 79085 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403493 69792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403454 71743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403522 124058 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 124058 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 125191 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 125191 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126774 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126774 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403474 127226 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 127226 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403505 133570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403445 166377 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 166377 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403468 168430 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 168430 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403493 69792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403523 70419 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70419 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403528 70545 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70545 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403513 134279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 134279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44394799 66254 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 66254 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
44394948 66245 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184585 66245 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405459 133156 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 133156 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
9895868 69582 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69582 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403477 71828 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71828 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44424072 85624 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85624 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
71719524 87785 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
CHEMBL2337750 87785 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
10421933 124645 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL364104 124645 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695914 73557 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73557 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417936 81592 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216323 81592 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
71720121 87791 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
CHEMBL2337756 87791 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
44403473 70480 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
CHEMBL194630 70480 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
70689595 73561 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73561 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73550 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73550 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70695859 73502 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73502 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
11272081 81458 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215964 81458 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71732074 131246 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686774 131246 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730664 131321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686849 131321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759587 131326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686854 131326 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
44417899 141573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
CHEMBL384919 141573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
11563383 70515 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70515 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
70681216 73613 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73613 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184672 122447 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600979 122447 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
54585863 60643 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60643 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23593468 64704 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64704 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89690864 139439 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 139439 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267714 196036 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL560283 196036 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
45267430 194813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
CHEMBL538993 194813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
49865654 16043 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 16043 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
24952055 91520 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91520 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10070680 72109 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 72109 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394604 125050 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 125050 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394807 66218 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 66218 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44417975 141860 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141860 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
71718317 87787 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337752 87787 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
127025096 138227 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 138227 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
23593472 64705 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64705 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
117798688 139468 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 139468 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89691193 139410 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 139410 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44408081 75057 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203549 75057 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407934 75931 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205112 75931 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
25114724 60795 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761126 60795 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
70695854 73470 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73470 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73511 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73511 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442062 94394 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250926 94394 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44562480 185906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL486878 185906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
70681115 73460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
89790062 131236 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686764 131236 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730918 131238 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686766 131238 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44417873 81459 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81459 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
6621104 66801 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL185997 66801 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
11634230 70174 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 70174 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184705 122501 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601046 122501 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
44193625 122547 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601375 122547 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
71714121 122549 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122549 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
9844702 64707 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64707 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11510887 82269 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 82269 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442118 94310 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250530 94310 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11577588 195839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL558442 195839 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666267 109378 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 109378 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11662906 73479 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73479 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11684745 16091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 16091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44408028 140904 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140904 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70691333 77972 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77972 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
44405487 71875 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71875 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691723 73566 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73566 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
21062991 64701 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64701 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
69603769 73450 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73450 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44403491 71767 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196686 71767 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403516 70294 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 70294 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
11204090 69836 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193771 69836 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403750 133913 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
CHEMBL371576 133913 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
70691737 73616 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73616 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70689519 73457 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73457 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562521 186760 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488886 186760 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
155562407 175207 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4571110 175207 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
71226938 129189 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
CHEMBL3670646 129189 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
71226243 129196 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
CHEMBL3670652 129196 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
71731050 131279 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686808 131279 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
10389978 69614 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69614 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21062990 64700 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64700 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798744 139473 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 139473 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
11713742 93563 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93563 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44408013 75056 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 75056 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
44143499 187927 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
CHEMBL496815 187927 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
45272014 195318 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551543 195318 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
18435988 74883 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031725 74883 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
70695855 73476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11613073 75930 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75930 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939881 64708 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818789 64708 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798680 139377 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 139377 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135486 91521 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91521 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
73356649 91531 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403870 91531 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
22421749 66306 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
CHEMBL184860 66306 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
11620005 81456 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81456 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397048 67437 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL188991 67437 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44442061 94359 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250730 94359 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
17545006 175236 4 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
CHEMBL4571855 175236 4 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
17173466 175243 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4572083 175243 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
44442093 94269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL250311 94269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
70693793 73554 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73554 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562416 176966 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462352 176966 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
45271103 195276 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551281 195276 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
70687478 73501 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73501 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
9848699 60638 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL176024 60638 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44417904 80377 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL214432 80377 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
71730661 122546 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601374 122546 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759544 131243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686771 131243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759585 131319 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686847 131319 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730916 131330 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686858 131330 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
10344176 67185 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 67185 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25115856 60788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761118 60788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184696 122491 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601037 122491 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89690396 138252 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 138252 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71730661 122546 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601374 122546 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
1314 3727 21 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3727 21 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3727 21 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
11640515 80509 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80509 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
20817762 77325 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 77325 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11640515 80509 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80509 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
11975327 141761 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
CHEMBL386021 141761 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
44143494 184254 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
CHEMBL483673 184254 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
53318801 56701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
49865679 16061 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 16061 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10250850 72411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72411 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11419666 122553 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122553 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
44394855 67280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 67280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
44405412 71874 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71874 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44417982 82512 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82512 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
89690239 138207 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 138207 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025110 138291 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 138291 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
89690292 138188 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 138188 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691193 139410 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 139410 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44403548 70392 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70392 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
11656044 141137 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 141137 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10319824 67081 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 67081 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
44407710 73940 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73940 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70689596 73563 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73563 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695915 73567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394973 66227 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184528 66227 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
122184570 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600825 122420 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
22421750 70390 7 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194530 70390 7 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
91759582 131314 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686842 131314 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730790 131325 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686853 131325 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
71731049 131328 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686856 131328 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
16665072 98538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
44417917 82096 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 82096 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
89690607 138177 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 138177 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184885 122545 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601373 122545 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
11419666 122553 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
CHEMBL360142 122553 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
11635187 195734 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557263 195734 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
18436123 74875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
CHEMBL2031717 74875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
44562564 189138 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 189138 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
56597991 139176 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 139176 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11511219 66135 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 66135 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407991 169453 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 169453 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394864 126198 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 126198 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
9955811 66171 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 66171 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394986 123338 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL361654 123338 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11452268 81573 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81573 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
54580457 60579 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60579 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
56673714 64720 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64720 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
22422406 67452 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
CHEMBL189083 67452 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
11583925 165771 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165771 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11342160 122935 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360671 122935 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11342160 122935 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL360671 122935 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44394972 66201 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184418 66201 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
22421743 66823 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL186077 66823 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
122184687 122483 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601024 122483 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
70687470 73461 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73461 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442068 94361 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250746 94361 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
122184674 122450 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
CHEMBL3600982 122450 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
44407479 73663 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL201813 73663 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
11662657 81124 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 81124 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
70685346 73497 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73497 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
86695564 131228 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686756 131228 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730532 131234 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686762 131234 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71731945 131251 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686779 131251 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759556 131261 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686789 131261 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730921 131263 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686791 131263 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732075 131265 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686793 131265 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
71730135 131280 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686809 131280 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759580 131312 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686840 131312 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759589 131331 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686859 131331 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
44417995 82441 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82441 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57402993 69633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934825 69633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70687552 73621 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73621 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89691439 138248 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 138248 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
11740891 122470 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601012 122470 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89691439 138248 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3770359 138248 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
90469437 121270 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 121270 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438755 93503 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93503 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
45271829 195281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551332 195281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11634886 196665 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL564501 196665 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
18436125 74877 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031719 74877 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
11165058 154632 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154632 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
44562600 173131 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 173131 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11155432 82487 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82487 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
45267565 196285 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562073 196285 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11678370 136565 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136565 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44403484 70588 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194950 70588 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
49865790 16142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 16142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
59135479 91512 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403851 91512 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
15987638 126778 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
CHEMBL365374 126778 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
44562544 173841 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
CHEMBL453886 173841 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
49865708 16089 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 16089 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
91759577 131307 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686835 131307 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
57396022 69643 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934836 69643 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397820 69648 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934840 69648 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44143497 184112 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
CHEMBL482636 184112 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
45267739 196555 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
CHEMBL563791 196555 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
90666263 109374 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 109374 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
11531660 135594 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135594 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
12020156 196282 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL562016 196282 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
70685397 73564 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73564 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
127025110 138291 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 138291 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
70683237 73453 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73453 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44417942 82453 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217560 82453 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44401395 135986 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL373157 135986 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
90666254 109364 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 109364 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
44408099 75703 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204798 75703 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407950 140555 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL381143 140555 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
71717086 87788 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337753 87788 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
71714121 122549 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601377 122549 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
71730533 131310 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686838 131310 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
89690379 138180 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 138180 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89690318 138306 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 138306 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44193624 122530 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601299 122530 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691162 139371 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 139371 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
71660915 139413 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 139413 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273777 195852 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL558532 195852 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
44442121 94275 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
CHEMBL250326 94275 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
45270841 196733 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
CHEMBL565073 196733 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
11563017 81062 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 81062 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11713027 81174 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 81174 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
23567290 63474 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179872 63474 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44405488 133012 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
CHEMBL370222 133012 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
44405488 133012 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
CHEMBL370222 133012 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
70695929 73615 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73615 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
21940052 64711 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64711 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
57401531 68152 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914855 68152 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
44397606 124072 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL363256 124072 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
90666253 109363 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 109363 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
71731943 131247 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686775 131247 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759547 131250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686778 131250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
11568782 71899 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71899 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
11705485 168534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 168534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11511219 66135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 66135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11655872 71717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
25115621 60769 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761099 60769 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
60130302 122361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600390 122361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
89691162 139371 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 139371 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691065 139461 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 139461 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
16739263 93414 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 93414 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11712898 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL472363 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23657037 94524 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94524 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44442071 154614 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154614 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11712898 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11712898 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL472363 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 179188 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
44562500 186735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
45487330 198652 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL579232 198652 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
11656489 16141 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223968 16141 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11511219 66135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 66135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70695917 73572 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73572 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44401508 69821 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL193666 69821 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
44401552 165906 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL425012 165906 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
11604236 176701 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL459897 176701 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
44388559 60719 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60719 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44402768 69802 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL193583 69802 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44442060 154807 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400297 154807 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44397454 124103 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL363337 124103 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44424070 85751 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85751 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
11520239 3632 11 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3632 11 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3632 11 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
44394698 66241 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 66241 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
10360874 64934 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64934 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
11662657 81124 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 81124 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11554412 97021 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
CHEMBL266725 97021 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
10150955 80919 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80919 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 82300 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 82300 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141797 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141797 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71461 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71461 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25113835 60776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761106 60776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116082 60787 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761117 60787 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
16745235 122438 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600970 122438 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
122184695 122490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601036 122490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
127029624 138190 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 138190 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
57403784 68855 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68855 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
57890370 122407 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600812 122407 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184561 122410 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600815 122410 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11649549 93938 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93938 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11619850 75776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
CHEMBL204828 75776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
11619850 75776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75776 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
22348261 77063 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 77063 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
11775505 141987 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141987 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
44442053 154908 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400883 154908 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
24808474 91522 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91522 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952765 91527 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91527 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
71226964 129181 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 129181 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81566 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11598355 141803 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141803 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44397476 67426 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67426 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
11553316 71634 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71634 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11340348 129460 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL367156 129460 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
44143503 188069 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497830 188069 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44408027 75067 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 75067 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
18436119 76382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11222404 195378 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 195378 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487383 196982 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566662 196982 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
23593464 64702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
58646147 79085 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 79085 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522945 76385 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76385 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
57522468 76394 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76394 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
1305 511 14 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
9934033 511 14 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
CHEMBL182150 511 14 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
11570040 77769 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL209109 77769 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10027853 71862 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71862 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23593464 64702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23120540 196139 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 196139 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487652 199734 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL593521 199734 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
45487283 197471 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
CHEMBL569852 197471 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
45487309 197805 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572090 197805 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
21939950 64727 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64727 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44407710 73940 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73940 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407875 75062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 75062 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436112 74847 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031578 74847 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
11583744 71724 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71724 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
127029623 138335 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 138335 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522950 76390 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76390 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
53321223 56718 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
CHEMBL1642487 56718 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
57399740 68084 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 68084 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
71731807 131245 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686773 131245 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730394 131295 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686824 131295 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759584 131308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 131308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730659 131316 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686844 131316 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44405415 72569 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72569 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
44405486 140512 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 140512 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394860 66248 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 66248 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394606 67253 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 67253 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169096 87760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337725 87760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396019 69626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934819 69626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401250 69631 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934823 69631 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401252 69649 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934841 69649 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54584181 60775 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761105 60775 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70693807 73602 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73602 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690365 138175 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 138175 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54585864 60645 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60645 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
21108118 68156 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914859 68156 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45273623 195634 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL556296 195634 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44143498 187784 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
CHEMBL495789 187784 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
45271642 195155 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550308 195155 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45487366 197781 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL571830 197781 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
6621104 66801 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL185997 66801 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
44397262 67508 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67508 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403480 70550 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70550 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403506 71134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 71134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403474 127226 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 127226 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403468 168430 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 168430 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
20779426 60549 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175874 60549 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
44417892 80236 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
CHEMBL213771 80236 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
71720118 87770 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337735 87770 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25114948 60794 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761125 60794 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
45267654 196081 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL560677 196081 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
9828622 96654 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
CHEMBL263702 96654 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
44397175 126388 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL365094 126388 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
11330800 82274 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL217132 82274 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11569340 71650 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71650 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562543 173839 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL453885 173839 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
70681117 73465 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73465 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44402593 71611 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196332 71611 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
44562499 186734 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488720 186734 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
44394774 67212 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187859 67212 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45272040 195107 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL549930 195107 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
71731944 131249 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686777 131249 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732077 131269 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686797 131269 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759583 131315 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686843 131315 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44424069 85730 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85730 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424071 142097 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 142097 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
70687551 73617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117798744 139473 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 139473 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438747 93374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 93374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11974231 82420 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 82420 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
11511776 189300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 189300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11570031 73498 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73498 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408117 139559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11778029 66209 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 66209 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
71717084 87780 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337745 87780 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44562542 173227 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452335 173227 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
11597758 195172 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550455 195172 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71731948 122529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601298 122529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759581 131313 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686841 131313 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
22254604 123876 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123876 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
25115173 60782 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761112 60782 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
70691738 73622 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73622 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11569300 82482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
23022394 76380 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76380 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
59135478 91519 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91519 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11296279 80551 1 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL214858 80551 1 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71719522 87768 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337733 87768 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
45268457 196138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561133 196138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
49865738 16116 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 16116 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417017 80380 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 80380 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397480 67371 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
CHEMBL188655 67371 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
44397215 67507 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189492 67507 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
44390752 122996 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360876 122996 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394925 66184 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184353 66184 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
137635978 156056 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 156056 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
70681116 73463 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73463 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666258 109368 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219267 109368 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
137635978 156056 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 156056 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
10353807 66349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185096 66349 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
22427041 70311 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194417 70311 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
70689526 73507 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73507 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408014 75392 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203929 75392 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71731948 122529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601298 122529 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64724 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64724 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
122184566 122415 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600820 122415 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44407711 75932 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75932 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
44442151 94006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 94006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44407944 166002 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 166002 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11677277 141779 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141779 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
44405409 72400 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
CHEMBL198692 72400 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
45270147 195394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL552010 195394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11583925 165771 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165771 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397636 67203 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187814 67203 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
49865977 16218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11568741 196069 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560584 196069 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71226289 129191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670648 129191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
91759559 131266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686794 131266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732076 131267 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686795 131267 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730791 131327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686855 131327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
57396021 69636 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934828 69636 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690957 139325 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 139325 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691535 139382 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 139382 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
89691247 139408 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 139408 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44410878 78108 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 78108 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
45487392 196985 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566674 196985 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666098 109331 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 109331 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11454184 71089 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL195319 71089 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
71717700 87792 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337757 87792 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
59135490 91514 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403853 91514 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
11563153 136566 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136566 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 80403 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 80403 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
70691720 73553 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73553 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11705485 168534 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 168534 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44562479 186731 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488711 186731 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
10244148 66239 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
CHEMBL184573 66239 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
91759572 131296 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686825 131296 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71731047 131302 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686830 131302 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
91759584 131308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 131308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
11153928 165780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
59835766 122419 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600824 122419 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89690864 139439 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 139439 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
86582974 121268 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 121268 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117816804 121269 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 121269 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
45270139 195297 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL551408 195297 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
11533195 195745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557329 195745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
18435984 74880 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
CHEMBL2031722 74880 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
11292322 154411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398864 154411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49865680 16062 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 16062 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 16117 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 16117 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44390733 62494 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL178084 62494 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
21939887 64709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818790 64709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44417960 81796 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL216429 81796 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
44394997 64556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL181492 64556 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
1562 899 13 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
5312114 899 13 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL17645 899 13 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL195380 899 13 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
11974034 82097 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL216577 82097 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
70687537 73551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
70691656 73508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442050 94247 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250118 94247 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
71731946 131257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686785 131257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759557 131262 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686790 131262 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
10466405 123877 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362720 123877 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44418009 81863 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81863 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
70683287 73571 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73571 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184564 122413 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600818 122413 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
86582974 121268 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 121268 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45271114 195363 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL551886 195363 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
70691650 73458 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73458 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184569 122418 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600823 122418 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
24952419 91529 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403868 91529 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10399494 66503 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL185235 66503 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11581666 75928 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
CHEMBL205106 75928 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
44143490 192678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL521903 192678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
11246373 94308 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250528 94308 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759558 131264 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686792 131264 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759560 131268 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686796 131268 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89690365 138175 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 138175 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54579973 60642 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60642 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89691247 139408 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 139408 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562563 174360 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 174360 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11555572 196203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL561463 196203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
44394939 66152 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184205 66152 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403454 71743 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71743 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403445 166377 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 166377 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44424073 85625 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85625 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44417907 81472 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215989 81472 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44143489 187949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL497005 187949 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
71226696 129195 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670651 129195 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
71731046 131233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686761 131233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
71731947 131259 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686787 131259 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
11589812 81562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216180 81562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
10126754 81557 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81557 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59691557 122442 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600974 122442 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
90469437 121270 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 121270 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
117816748 139423 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 139423 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
71660914 139312 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 139312 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45272853 195733 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557262 195733 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
11634823 16139 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223966 16139 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44424067 143187 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 143187 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44390787 122565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360159 122565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394705 125321 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 125321 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11397595 124616 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL364071 124616 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
57392548 69641 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934833 69641 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
21939940 64710 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818791 64710 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939935 64713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818796 64713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690368 139496 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
CHEMBL3794523 139496 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
11591542 80403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 80403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
20779429 60545 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL175860 60545 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
91759554 131258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686786 131258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89691535 139382 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 139382 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11974346 141500 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 141500 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11712583 195167 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550410 195167 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
11719912 195886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
CHEMBL558928 195886 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
44442156 154388 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398748 154388 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11706442 195806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL558052 195806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127030071 139177 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 139177 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
127031356 139191 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 139191 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11440762 82141 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 82141 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
44403533 71456 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71456 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44395021 66207 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184439 66207 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11974132 80205 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
CHEMBL213658 80205 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
44408013 75056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 75056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
70693796 73568 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73568 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11464405 80496 26 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214731 80496 26 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11662657 81124 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 81124 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11510399 81548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216104 81548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417847 82435 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82435 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417911 82439 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82439 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418002 82565 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82565 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10456755 71098 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 71098 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114287 60574 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1760012 60574 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114067 60790 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761120 60790 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685409 73608 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73608 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184671 122446 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600978 122446 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184699 122495 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601040 122495 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
59835780 122480 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601021 122480 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835879 122482 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
CHEMBL3601023 122482 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
44438750 93413 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 93413 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11442761 140183 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
CHEMBL380429 140183 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
10075375 76002 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 76002 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
20817761 77268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 77268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
45268470 196295 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 196295 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
23120586 196737 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 196737 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
44143495 184255 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 184255 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
45270802 195078 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL549635 195078 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866036 16231 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16231 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44403517 71517 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71517 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
20817800 70417 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70417 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
9910346 64732 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64732 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10050565 75705 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75705 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436120 74879 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74879 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
53322555 56707 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642474 56707 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
23022536 76384 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76384 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
11634230 70174 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 70174 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23022509 76381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76381 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417821 80559 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80559 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
57403785 68862 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68862 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23120512 195308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 195308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
57522704 76377 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76377 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
24780883 56713 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56713 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
45487284 197661 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570987 197661 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10173726 80845 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80845 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57396294 68088 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 68088 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390750 63478 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL179878 63478 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
56666755 64722 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64722 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
45273703 195779 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557731 195779 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45487657 198993 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL585509 198993 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
44390778 64279 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL180962 64279 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
57392824 68083 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 68083 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44407836 75266 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 75266 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11635274 138688 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377843 138688 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
44417999 82206 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 82206 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
23120564 196545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563725 196545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45271839 196547 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 196547 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
155531314 171612 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4465399 171612 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
45487391 199028 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL585879 199028 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
9807658 64546 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181466 64546 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
155538229 172369 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4476156 172369 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
91759543 131241 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686769 131241 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
44405645 72465 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198890 72465 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405468 133432 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 133432 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44405518 140359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 140359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394569 66217 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 66217 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11281523 81802 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81802 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
44418010 81563 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216184 81563 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169097 87761 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337726 87761 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57390738 69619 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934812 69619 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57395050 68856 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68856 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
52917998 60632 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60632 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683781 74950 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032047 74950 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
71660915 139413 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 139413 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45271111 195334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551684 195334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
45273401 195773 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL557715 195773 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
24952056 91518 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91518 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
127031354 139105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 139105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627122 141738 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141738 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44407860 75421 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75421 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407870 75914 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75914 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403467 70542 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70542 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403505 133570 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133570 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44402350 72028 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197571 72028 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
11678370 136565 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136565 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417824 141851 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386509 141851 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11410594 97201 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL268385 97201 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11562129 71077 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 71077 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44394826 66605 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66605 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10083869 65574 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11201645 71871 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71871 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
70687549 73610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693808 73619 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73619 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44193451 122528 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601297 122528 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691065 139461 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 139461 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143502 187983 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497221 187983 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562404 176964 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176964 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
11706443 196223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
CHEMBL561585 196223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
44402484 133530 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL370839 133530 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11282448 62575 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62575 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
60168817 87774 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337739 87774 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690239 138207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 138207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44403547 133614 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371355 133614 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403500 135214 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL372245 135214 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44442054 94273 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250321 94273 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
45268644 196217 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL561546 196217 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
71716477 87779 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337744 87779 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11662564 133526 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 133526 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
137644041 158449 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 158449 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
45269996 196421 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562905 196421 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
137644041 158449 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 158449 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
25114064 60785 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761115 60785 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
89690318 138306 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 138306 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574358 178708 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468299 178708 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
44574359 178735 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468509 178735 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11634061 192353 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 192353 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
127033945 138953 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138953 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407991 169453 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 169453 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71225876 129192 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
CHEMBL3670649 129192 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
122184568 122417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600822 122417 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
57394273 69639 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934831 69639 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44408013 75056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 75056 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
137657882 159674 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159674 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
137657882 159674 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159674 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
11973798 80298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
CHEMBL214075 80298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
44143501 187982 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
CHEMBL497220 187982 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
44417910 82428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL217435 82428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417992 82457 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82457 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71932 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71932 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
117816804 121269 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 121269 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
89691032 139441 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 139441 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562442 179189 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 179189 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
155524512 170966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
CHEMBL4455933 170966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
44397033 67140 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187553 67140 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
702501 157584 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4080696 157584 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
22254575 66322 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184980 66322 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
10198125 126644 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365254 126644 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44403748 70625 4 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
CHEMBL194997 70625 4 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
11527169 77379 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL208635 77379 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
89691416 139460 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3794147 139460 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
45269336 195982 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 195982 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407956 74861 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74861 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11627085 195411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL552143 195411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44405517 71861 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197023 71861 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
71718319 87795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337760 87795 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44403749 166221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL426648 166221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
45267386 196009 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560063 196009 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
71227161 129187 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
CHEMBL3670644 129187 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
44417848 141622 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141622 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
11516903 70280 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194253 70280 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
70681217 73620 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73620 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70693809 73623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89691032 139441 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 139441 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45487641 199029 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585880 199029 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
70691649 73455 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73455 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865653 16042 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 16042 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
57402500 68154 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
CHEMBL1914857 68154 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
46899579 16990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253956 16990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44402599 126185 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL364936 126185 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
52918017 60647 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60647 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
57391045 68148 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 68148 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11419338 74446 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
CHEMBL202741 74446 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
45270303 196626 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL564243 196626 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
90666260 109370 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 109370 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
89691216 139401 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 139401 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11563153 136566 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136566 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417938 97338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
CHEMBL269352 97338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
89690379 138180 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 138180 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691144 139445 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 139445 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974131 141986 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141986 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
70687473 73474 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73474 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184559 122402 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600808 122402 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
66877080 91530 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403869 91530 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
44394910 67007 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186947 67007 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44407967 74492 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74492 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
11591169 71746 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71746 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
44407667 74406 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74406 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
71731804 131242 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686770 131242 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71660914 139312 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 139312 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45268465 196561 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 196561 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18435986 74882 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031724 74882 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
11554989 179063 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 179063 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44407667 74406 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74406 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
57391030 68092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914648 68092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10258364 194784 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
44395022 166154 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL426252 166154 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44442069 154811 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400321 154811 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
91759575 124392 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3639387 124392 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
45272816 195789 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL557873 195789 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
70693732 73462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73462 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44418008 81854 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL216454 81854 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44397278 67302 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188340 67302 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
22254580 67008 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186949 67008 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
44417963 166011 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL425445 166011 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
44405464 166351 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 166351 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44394856 66134 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 66134 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394824 124268 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 124268 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394611 124347 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 124347 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 124347 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 124347 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
16721015 80421 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80421 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11495432 98199 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL274168 98199 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018932 80306 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 80306 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018914 80915 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80915 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417956 96651 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96651 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
10388797 71759 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71759 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57392547 69634 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934826 69634 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25115855 60772 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761102 60772 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116079 60781 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761111 60781 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114722 60792 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761123 60792 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184563 122412 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600817 122412 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835728 122425 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600830 122425 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978428 122469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601011 122469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388351 122475 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601017 122475 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11408441 141255 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
CHEMBL383078 141255 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
44410823 75554 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75554 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348219 76524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
20817821 76859 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76859 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410821 77123 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 77123 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11259253 82545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82545 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
44442144 154695 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154695 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45270014 195113 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
CHEMBL549984 195113 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
45487372 196915 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566232 196915 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
9829942 66170 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
CHEMBL184291 66170 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
11236807 81566 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563017 81062 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 81062 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11613073 75930 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75930 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44390715 123820 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362400 123820 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
53325164 56717 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56717 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
11752320 67732 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL190780 67732 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
57398088 68082 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 68082 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45487390 197086 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL567514 197086 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
44394907 165992 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165992 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
23593464 64702 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23593464 64702 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939902 64719 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64719 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
44408108 139814 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139814 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57521366 76395 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76395 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407944 166002 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 166002 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10186375 78948 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL2112988 78948 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
11683259 195766 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557664 195766 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45267577 195968 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 195968 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487331 198802 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL583348 198802 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10141528 122950 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL360731 122950 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
4219492 71437 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71437 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
56673713 66455 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66455 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66455 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
1314 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9865843 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
CHEMBL178707 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9978508 188040 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497637 188040 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522949 76389 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76389 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
1314 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
9865843 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
CHEMBL178707 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
1314 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
9865843 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
CHEMBL178707 3727 21 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
56589628 68149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 68149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
23120576 195778 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557730 195778 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11654412 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11654412 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 198918 26 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
57522947 76387 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76387 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
44407991 169453 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 169453 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417944 141810 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141810 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11502008 56572 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56572 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11512135 70308 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 70308 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
10024171 188045 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 188045 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
53317306 56705 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56705 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45487382 197397 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL569458 197397 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
59135482 91523 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91523 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44390706 122033 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL359510 122033 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11612403 71410 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195914 71410 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10185187 63299 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179325 63299 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
71730133 131274 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686803 131274 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
89798653 131305 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686833 131305 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
9806086 65207 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 65207 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
10434776 126382 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 126382 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394959 67210 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 67210 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405570 71992 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71992 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405408 72434 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72434 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405463 133157 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370361 133157 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
10083869 65574 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65574 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394859 66246 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 66246 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394573 123682 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123682 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
11591169 71746 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71746 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
60169184 87765 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337730 87765 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169263 87767 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337732 87767 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71719525 87786 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337751 87786 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
57396020 69635 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934827 69635 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394275 69645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934838 69645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54586089 60774 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761104 60774 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
56683679 64723 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64723 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44442135 154425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398964 154425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11511219 66135 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL184084 66135 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11496313 72312 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL198361 72312 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
59135471 91513 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91513 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11304816 66279 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
CHEMBL184717 66279 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
44397008 66902 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66902 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44397127 67083 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 67083 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44397026 127170 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 127170 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44403528 70545 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70545 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403499 71117 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 71117 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403522 124058 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 124058 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 125191 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 125191 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44442056 94307 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250527 94307 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44402549 71798 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196781 71798 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
70681213 73603 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73603 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44438745 93858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
53325165 56719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642488 56719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
71716479 87793 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337758 87793 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397120 66889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL186417 66889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44403472 71729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
155522708 170786 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4452982 170786 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44442100 154688 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
CHEMBL399712 154688 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
101007561 156389 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 156389 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
101007561 156389 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 156389 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44397099 67111 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
CHEMBL187413 67111 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
11510669 189299 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 189299 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
44394638 123799 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123799 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
49865869 16177 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 16177 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
86695569 131239 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686767 131239 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
91759546 131248 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686776 131248 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759563 131277 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686806 131277 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
22254582 66972 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66972 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11973801 141968 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141968 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
10480652 65321 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 65321 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394607 124353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 124353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
70685395 73546 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73546 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
11599681 70344 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194484 70344 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54583209 60791 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761122 60791 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
91759590 131333 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686860 131333 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
70687538 73574 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73574 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690607 138177 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 138177 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574357 178707 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468298 178707 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
44442097 94010 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 94010 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44394908 67209 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187850 67209 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
71720119 87781 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337746 87781 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
46899581 17006 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254141 17006 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11620005 81456 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81456 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 80403 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 80403 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
44402419 71673 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196390 71673 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
45267385 194935 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL541944 194935 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
90666256 109366 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 109366 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
10083869 65574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695916 73570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11270984 63768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL180168 63768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11270984 63768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
CHEMBL180168 63768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
5817261 70326 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194468 70326 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
25114065 60780 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761110 60780 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
59135485 91516 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403855 91516 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44403483 70376 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194521 70376 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44390456 64901 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
CHEMBL182235 64901 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
71716480 87794 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337759 87794 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11974233 82142 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 82142 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
49866087 16243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16243 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
44408020 75432 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL204168 75432 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
91759588 122533 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601302 122533 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
54579974 3240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
91759588 122533 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601302 122533 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
11525369 141254 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
CHEMBL383076 141254 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
11974229 82483 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82483 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
45272837 195880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558863 195880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44442065 94311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 94311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24952417 91515 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91515 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44442066 94312 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250541 94312 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
71226436 129190 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
CHEMBL3670647 129190 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
91759574 131304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686832 131304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
11304816 66279 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
CHEMBL184717 66279 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
44442130 94191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249714 94191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44394684 127295 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL365876 127295 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
10353806 66904 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186481 66904 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44395001 66265 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184658 66265 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390369 64610 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181727 64610 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44402433 135218 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372291 135218 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
91759564 131278 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686807 131278 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759573 131303 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686831 131303 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
4219492 71437 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71437 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11974130 80362 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 80362 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394944 64875 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182161 64875 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
45267399 196684 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564674 196684 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
44405482 71851 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71851 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394792 124740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
9799244 80585 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80585 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018997 141708 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141708 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57397819 69646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934839 69646 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
122184693 122487 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601033 122487 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10433825 122400 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600806 122400 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
60130337 122409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600814 122409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9824856 122424 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600829 122424 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11504274 122467 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601009 122467 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
10024145 122471 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601013 122471 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11328029 76530 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
CHEMBL206081 76530 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
45273642 196455 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 196455 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
11599973 194897 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 194897 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
11599186 73499 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73499 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56597407 139054 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 139054 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030069 139108 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 139108 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
11648912 80351 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 80351 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
44403467 70542 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70542 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403518 71764 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71764 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11560917 124052 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 124052 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10389978 69614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69614 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44403765 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
23593464 64702 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56666755 64722 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64722 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44408109 75543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
127029624 138190 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 138190 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
45487673 197280 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568572 197280 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10344176 67185 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 67185 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
21940008 64725 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64725 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57396294 68088 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 68088 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44418003 82468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82468 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
21108056 68080 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 68080 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18435980 74884 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
CHEMBL2031726 74884 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
11596311 56716 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56716 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
57401509 68087 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 68087 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44143496 192087 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 192087 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
53318593 56710 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56710 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
57522704 76377 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76377 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57522816 76383 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76383 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
155516949 170152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4444299 170152 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71816518 138284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 138284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
56680348 64721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23120575 195873 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 195873 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
45487653 199007 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 199007 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
53318594 56723 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642492 56723 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390768 64474 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181383 64474 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403765 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135860 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
9824428 66257 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 66257 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394764 123169 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 123169 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
22254581 66225 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 66225 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44417856 80840 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80840 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169098 87762 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337727 87762 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169182 87764 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337729 87764 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25116309 60783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761113 60783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
11975438 80232 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 80232 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44397128 124102 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 124102 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44403501 69650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44403524 71465 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71465 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11611530 134805 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134805 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
89691216 139401 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 139401 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44401671 70266 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194173 70266 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10466478 124028 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL363011 124028 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695918 73575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57390252 68153 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 68153 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
45273659 195832 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 195832 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44442124 154893 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400799 154893 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11583925 165771 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165771 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563153 136566 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136566 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44402414 71406 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195896 71406 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
10443853 66216 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184476 66216 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45270273 195587 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL555349 195587 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
70689594 73547 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73547 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
127025395 138281 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 138281 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
57399742 68093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914651 68093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9999058 94306 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250526 94306 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
70693794 73558 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73558 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
70685398 73576 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73576 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45273783 195866 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558726 195866 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
45273790 195922 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL559329 195922 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
59135479 91511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403850 91511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44407967 74492 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74492 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
10389430 125951 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL364863 125951 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
59691584 122444 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600976 122444 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
70687479 73510 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73510 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562481 186011 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL487041 186011 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70695860 73416 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016580 73416 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56683679 64723 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64723 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44438742 93825 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247689 93825 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11374857 80219 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 80219 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
44394921 66240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 66240 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
44394961 67235 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL187953 67235 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
10038053 66108 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183932 66108 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
53321222 56711 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642478 56711 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
49865975 16215 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16215 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10456755 71098 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 71098 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
117798675 139360 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 139360 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
71660917 139374 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 139374 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11464405 80496 26 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80496 26 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
44250211 196222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL561584 196222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127029632 138322 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 138322 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
53317524 56714 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642483 56714 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
17484866 66840 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
CHEMBL186159 66840 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
90666261 109372 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 109372 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70681215 73612 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73612 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11975326 80508 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80508 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
45270319 195221 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550816 195221 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44562565 174071 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL454424 174071 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
45272539 195911 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
CHEMBL559237 195911 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
44394587 124065 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363220 124065 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
22421739 67116 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL187430 67116 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
86695565 131229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686757 131229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759584 131308 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 131308 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759578 131334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686861 131334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45270850 196654 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL564413 196654 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
59135474 91524 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91524 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
70695913 73549 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73549 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44401368 70259 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL194122 70259 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
49866086 16242 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16242 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70685410 73611 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73611 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
60130349 122396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600802 122396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44410904 172457 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 172457 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442063 94395 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 94395 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
49865678 16060 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 16060 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
44403478 166313 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427187 166313 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44388096 63510 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
CHEMBL180009 63510 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
70685408 73605 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73605 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
127028868 139342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3792826 139342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
70691648 73451 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016699 73451 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44407989 75380 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203858 75380 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
44405619 72504 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72504 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44394725 66151 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 66151 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
11719291 81898 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216482 81898 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
11711452 82036 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216554 82036 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
57394274 69642 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934834 69642 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25116307 60778 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761108 60778 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
16742746 122448 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600980 122448 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10274635 68859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
122184832 122525 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601294 122525 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
9978490 122423 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 122423 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44410838 77061 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 77061 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
53324076 56709 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56709 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
44442064 154808 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154808 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
45487384 196841 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 196841 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
70681113 73456 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73456 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691653 73481 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73481 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
71226400 129183 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 129183 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 139068 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 139068 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71226277 139119 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 139119 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81566 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11641948 80341 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 80341 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
11583747 81495 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81495 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
44403524 71465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11603897 124328 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 124328 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11548234 71196 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 71196 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45271907 195056 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL549512 195056 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44408028 140904 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140904 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57391028 68085 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 68085 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 68084 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 68084 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
21062998 64715 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64715 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690574 138325 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 138325 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57392824 68083 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 68083 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11532924 138382 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 138382 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
89690574 138325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 138325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53317307 56712 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56712 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
127029623 138335 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 138335 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522701 76396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76396 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
71226895 129188 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
CHEMBL3670645 129188 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
91759552 122532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3601301 122532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759551 131255 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686783 131255 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
44394909 67034 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 67034 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44405519 72371 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72371 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394605 67018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 67018 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394639 66706 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66706 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10361342 122924 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122924 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11188955 80467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
60168816 87772 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337737 87772 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759552 122532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601301 122532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64724 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64724 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798671 139356 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 139356 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
57401508 68086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 68086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
44403516 70294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 70294 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403480 70550 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70550 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403479 98208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 98208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403538 136111 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 136111 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403479 98208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 98208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403511 136173 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 136173 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
122184567 122416 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600821 122416 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11409615 141765 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL386039 141765 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
91759576 131306 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686834 131306 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
11178792 94525 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251702 94525 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45268247 196595 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564032 196595 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
44407629 168654 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168654 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11304816 66279 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL184717 66279 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
44394998 65173 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182466 65173 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11676200 179215 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472554 179215 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71718911 87797 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337762 87797 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759565 131281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686810 131281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
89690124 138299 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 138299 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691143 139315 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 139315 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44395019 66237 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 66237 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
60168914 87773 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337738 87773 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
22254540 67053 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL187165 67053 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
44407870 75914 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75914 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
89691144 139445 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 139445 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974230 166012 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 166012 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
18436129 74876 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
CHEMBL2031718 74876 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
44394596 66205 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 66205 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
22421743 66823 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186077 66823 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
70695852 73467 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016716 73467 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11546687 81555 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81555 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
25115852 60770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761100 60770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70681214 73606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117816748 139423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 139423 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
11635332 195073 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL549595 195073 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
25116306 60777 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
CHEMBL1761107 60777 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
11975436 79093 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 79093 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
11632909 133441 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 133441 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417898 82575 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL217860 82575 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
10202381 68858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44417890 165976 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL425257 165976 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
21939767 64698 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64698 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
89691019 139393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 139393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117816753 139337 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 139337 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798780 139391 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 139391 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135492 91526 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91526 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16721015 80421 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 80421 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
54583954 60635 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60635 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10386529 122473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601015 122473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
71660917 139374 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 139374 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
57396310 68150 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914853 68150 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
89690600 138179 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 138179 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
59835909 122476 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601018 122476 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11351174 140126 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL380144 140126 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11526309 189218 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 189218 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
11396908 71812 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL196839 71812 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
70695851 73452 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73452 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
10443307 66946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186659 66946 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
86695566 131230 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686758 131230 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
57401508 68086 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 68086 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
70689525 73506 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73506 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
10303307 64476 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181393 64476 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10073563 67535 6 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL189653 67535 6 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44394931 124037 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL363047 124037 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11531010 133588 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133588 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
15133403 206350 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 206350 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25113838 60784 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761114 60784 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184558 122399 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600805 122399 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184560 122403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600809 122403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
59835725 122426 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600831 122426 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835758 122481 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601022 122481 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
23593464 64702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
45271633 195546 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL554511 195546 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666097 109330 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 109330 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11591644 16090 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 16090 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522945 76385 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76385 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
44403517 71517 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71517 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
10436090 66206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 66206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
57401510 68090 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 68090 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45272701 195651 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL556432 195651 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
1305 511 14 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
9934033 511 14 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
CHEMBL182150 511 14 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
57522946 76386 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76386 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57522701 76396 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76396 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
23593474 64703 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64703 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939915 64716 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64716 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
57398088 68082 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 68082 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11582824 78093 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 78093 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
56673713 66455 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66455 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66455 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57401509 68087 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 68087 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44402329 71922 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL197210 71922 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11563383 70515 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70515 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
71730269 122535 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601304 122535 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
53317305 56704 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56704 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
24952419 91525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44143504 188070 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497831 188070 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45487653 199007 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 199007 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
44394572 66514 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66514 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394883 126364 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 126364 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169185 87766 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337731 87766 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60168818 87775 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337740 87775 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71720120 87784 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337749 87784 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690600 138179 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 138179 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
57390252 68153 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 68153 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
44442148 154696 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399734 154696 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44403472 71729 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71729 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
44417915 141389 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 141389 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
11632484 70334 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 70334 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
44407711 75932 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75932 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
22254570 66140 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184102 66140 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
70683299 73607 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73607 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45271994 195187 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL550535 195187 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
44401616 70033 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193970 70033 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
45273392 195740 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
CHEMBL557306 195740 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
10421932 67082 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187295 67082 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417934 82465 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL217605 82465 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
11496313 72312 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 72312 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
3611477 127514 8 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL366180 127514 8 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89690124 138299 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 138299 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
45272024 195412 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
CHEMBL552144 195412 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
44562415 176965 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176965 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44408109 75543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402505 71443 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196115 71443 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
44396196 66985 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186842 66985 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
10083101 66070 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183739 66070 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
89789910 131235 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686763 131235 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45267561 196585 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL563984 196585 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407711 75932 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75932 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
11204090 63507 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL180003 63507 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401449 71094 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195346 71094 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
10149893 81453 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215955 81453 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
91759555 131260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686788 131260 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
23593472 64705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70691651 73464 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73464 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442067 94313 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250544 94313 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
1314 3727 21 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3727 21 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3727 21 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11539632 70561 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70561 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89691057 139471 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 139471 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
10255474 123671 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123671 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44405477 72013 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197485 72013 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691724 73569 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73569 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44207909 16699 3 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16699 3 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16699 3 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16699 3 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
57391027 68079 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914628 68079 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391045 68148 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 68148 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44438753 93460 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93460 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
49865871 16179 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 16179 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44407956 74861 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74861 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417976 165942 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165942 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
49865976 16217 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16217 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44395082 66086 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL183839 66086 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
44442119 94249 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250122 94249 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
155520135 173243 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
CHEMBL4524539 173243 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
59691661 122445 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600977 122445 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730269 122535 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3601304 122535 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44405651 71930 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71930 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
44417844 141587 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141587 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141661 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141661 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25116308 60779 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761109 60779 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
122184697 122492 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601038 122492 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
9934161 74951 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032048 74951 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44410904 172457 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 172457 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442090 94160 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 94160 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
44442139 94458 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94458 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693733 73475 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73475 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
127030367 139063 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 139063 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 139161 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 139161 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597689 139166 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 139166 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11627122 141738 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141738 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44403477 71828 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71828 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403513 134279 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 134279 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403511 136173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 136173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403518 71764 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71764 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11545677 70377 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70377 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
89689924 138332 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 138332 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89702566 139328 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 139328 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11512135 70308 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 70308 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44390742 123290 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL361442 123290 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11559625 56715 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56715 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390713 123695 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362193 123695 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44573820 193268 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL523882 193268 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11627530 75910 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75910 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10005009 166376 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 166376 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
56666754 64714 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64714 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44573932 187491 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
CHEMBL494156 187491 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
22254551 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
44394592 65762 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65762 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
22254551 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
22254551 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 125044 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
71719526 87789 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337754 87789 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89691284 139422 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 139422 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117798671 139356 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 139356 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798692 139346 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 139346 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45273778 195853 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558533 195853 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23022394 76380 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76380 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44396952 66728 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66728 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397425 66877 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66877 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
44397221 67132 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 67132 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44403527 127175 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 127175 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403498 71078 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 71078 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
57403264 68076 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914625 68076 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
89691264 139487 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794445 139487 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143505 188041 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497638 188041 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562405 190907 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518514 190907 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
57390739 69640 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934832 69640 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691739 73624 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73624 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11974228 80372 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 80372 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
44407860 75421 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75421 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402567 165812 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL424836 165812 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
44394983 66280 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 66280 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
122184700 122496 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601041 122496 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
89690237 138224 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 138224 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44562403 189828 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189828 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
46902026 16971 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253789 16971 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44562462 179168 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472196 179168 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
91759550 131254 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686782 131254 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683300 73609 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73609 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
59691704 122443 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600975 122443 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
127025395 138281 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 138281 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
44407997 75388 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL203917 75388 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
44413259 139690 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
CHEMBL379802 139690 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
44417906 141410 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL384043 141410 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
44417864 80290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 80290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44403747 70586 6 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194946 70586 6 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
122184691 122484 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601030 122484 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89690622 138336 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 138336 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21939767 64698 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64698 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
127029631 138212 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769964 138212 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57401251 69632 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934824 69632 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70685336 73454 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73454 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394926 126260 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365011 126260 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390385 122516 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360117 122516 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417955 82434 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217460 82434 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
44562443 179190 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
CHEMBL472380 179190 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
11705240 132813 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132813 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
20817864 76060 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 76060 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
44402635 71854 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL196991 71854 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
127028869 139495 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3794501 139495 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
11974227 169305 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 169305 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
11635230 195576 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL555135 195576 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
127029632 138322 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 138322 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442070 154625 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399312 154625 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11520239 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
1313 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
CHEMBL185271 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
45273336 195762 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 195762 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 195762 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
45273336 195762 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 195762 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 195762 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
9915039 60823 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL176219 60823 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
10258364 194784 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
11520239 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
1313 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
CHEMBL185271 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
11520239 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
1313 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
CHEMBL185271 3632 11 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
45279585 123583 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123583 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
10118862 60802 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176159 60802 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
4033 1899 48 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1899 48 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1899 48 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
45279585 123583 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123583 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
45279490 123577 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123577 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10230490 63179 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178997 63179 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10258364 194784 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10118863 60819 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176208 60819 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44455336 95589 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
CHEMBL257733 95589 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
45279490 123577 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123577 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
45278579 123578 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123578 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10258364 194784 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 194784 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 194784 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
16043291 79993 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79993 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10004545 74952 7 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74952 7 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10324628 142225 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 142225 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 167363 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 167363 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
10209344 123254 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL361392 123254 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44416651 80397 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 80397 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416651 80397 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 80397 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
45278579 123578 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123578 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
46188603 121764 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121764 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
45279869 123587 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123587 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
10204151 165888 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL424961 165888 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10114686 60570 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175993 60570 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141840 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141840 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10186594 168561 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL435708 168561 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10226765 123136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
CHEMBL361215 123136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
10226765 123136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL361215 123136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141840 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141840 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430458 142811 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142811 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
11719447 66982 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL186827 66982 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397114 127550 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL366309 127550 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
11640865 77770 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209110 77770 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532402 139296 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379189 139296 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
10204047 60519 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175709 60519 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10231341 63346 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL179437 63346 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
11582824 78093 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 78093 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44424218 166045 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425654 166045 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52948857 19169 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
CHEMBL1289614 19169 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
10113523 129816 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL367532 129816 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11661999 77492 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208720 77492 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
10117415 60824 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176220 60824 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10298251 131375 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL368888 131375 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414520 80271 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 80271 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279869 123587 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123587 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
45279867 123602 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618363 123602 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
10369833 92567 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92567 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
10161039 60535 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175815 60535 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11307645 82128 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216681 82128 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11582825 78589 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL211223 78589 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
45279148 123593 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123593 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416800 96842 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96842 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 169371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 169371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 169371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 169371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44413240 79817 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
CHEMBL212053 79817 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
44414497 179144 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 179144 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 179144 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424212 85753 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229113 85753 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424213 85757 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229171 85757 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
10174940 141092 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382668 141092 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
10301472 124656 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364162 124656 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
11519451 140216 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL380509 140216 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
11635674 201849 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 201849 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45279402 123589 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123589 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
10437982 92571 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92571 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
10183297 93312 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 93312 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
11168186 68028 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
CHEMBL191393 68028 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
44416859 141527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 141527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11612046 77784 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209172 77784 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532214 138635 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377588 138635 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424215 137185 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374844 137185 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16755871 92495 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92495 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16755870 144486 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 144486 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756284 151486 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 151486 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
11168831 124036 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL363044 124036 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
44416859 141527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 141527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416670 141924 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141924 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
49869631 128101 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665347 128101 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
58093389 128134 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665379 128134 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
49870047 128160 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665404 128160 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
49868914 129804 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129804 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092307 129813 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675316 129813 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
44424062 85860 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229791 85860 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44455368 95630 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95630 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416970 80328 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 80328 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80511 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80511 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416898 141465 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384282 141465 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11719647 138907 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378309 138907 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44414518 77909 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77909 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 80181 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 80181 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
9986044 80846 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215259 80846 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16739324 149759 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149759 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44397031 126780 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL365400 126780 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425810 143417 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389809 143417 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
9985634 79757 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79757 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424214 85758 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229172 85758 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
11511671 141208 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382841 141208 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756185 149721 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149721 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756641 142589 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142589 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49868672 128064 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665310 128064 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
49868941 128074 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665320 128074 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49869071 128076 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665322 128076 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424195 85867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229822 85867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44415364 79832 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79832 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
50903065 131825 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131825 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
49869490 128095 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665341 128095 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
11752339 69399 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69399 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
49869347 128089 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665335 128089 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
10053937 80248 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 80248 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869493 128099 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665345 128099 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
44425828 166293 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL427107 166293 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756405 92867 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92867 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
10139873 80106 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213198 80106 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
23567513 62394 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177955 62394 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
44417830 80590 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
CHEMBL215005 80590 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
44415419 79790 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
CHEMBL211934 79790 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
44440593 149095 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394311 149095 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44416797 80604 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL215075 80604 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
21101416 141889 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386753 141889 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020151 195188 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550545 195188 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44440587 93647 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246790 93647 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389461 122625 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360327 122625 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
44416474 80390 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214499 80390 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
57524677 126413 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
CHEMBL3651089 126413 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
44389521 64563 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
CHEMBL181516 64563 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
57524582 126393 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651069 126393 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
45271219 195430 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
CHEMBL552292 195430 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
45279491 123575 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123575 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45271221 195463 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552498 195463 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
12020161 194811 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL538968 194811 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
44416310 96658 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
CHEMBL263771 96658 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
44437544 151727 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396448 151727 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437544 151727 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396448 151727 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
23567394 60874 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176230 60874 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
44415501 77945 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77945 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44440588 93595 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246590 93595 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389533 172436 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL447835 172436 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
20779413 60566 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175964 60566 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
20779393 123571 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL361821 123571 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49868664 129663 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673560 129663 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
49870454 128125 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665370 128125 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870576 128137 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665382 128137 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
58093397 128144 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665389 128144 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
58093339 128145 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665390 128145 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
49870706 128153 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665398 128153 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
49869331 129784 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675289 129784 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
44417905 82472 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82472 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44416970 80328 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 80328 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80511 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80511 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11546697 77366 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208551 77366 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
11758076 80044 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212941 80044 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
9851676 138539 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377519 138539 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415364 79832 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79832 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
10053937 80248 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 80248 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
46869326 65470 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830042 65470 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
56680482 65473 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830045 65473 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424217 85765 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229223 85765 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424186 166048 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425664 166048 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52942795 19172 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289619 19172 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
52941615 19188 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289722 19188 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
25205317 19317 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290593 19317 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11605821 141591 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL385011 141591 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11420543 67440 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL189029 67440 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
49869208 128083 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 128083 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
25054289 19086 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289054 19086 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
49868940 128073 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665319 128073 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
11785761 141400 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383976 141400 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11785261 67585 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL190068 67585 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
57988809 80500 14 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL2147472 80500 14 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
49869775 128104 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665350 128104 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49868805 128066 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665312 128066 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
49869488 128079 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665325 128079 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
50902183 124625 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640814 124625 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
44416840 141850 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL386507 141850 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44388277 63306 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179345 63306 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415501 77945 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77945 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44425792 85950 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL230082 85950 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
44388141 60501 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175581 60501 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49869916 128113 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665359 128113 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
11635674 201849 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 201849 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
1252415 154621 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
CHEMBL399302 154621 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
11238718 161494 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL412801 161494 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44414465 168376 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL434571 168376 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416357 166072 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425791 166072 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44425795 85951 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL230083 85951 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44416587 141416 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL384079 141416 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44424263 85787 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229406 85787 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
10311260 67262 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL188084 67262 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
45267849 196132 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL561092 196132 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
71450908 78949 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL2112989 78949 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
10483604 79836 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212142 79836 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
2881764 94573 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
CHEMBL251947 94573 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
49870184 128115 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665360 128115 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
66886358 128129 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665374 128129 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
58093414 128170 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665414 128170 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
49869049 129782 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675287 129782 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
49869051 129783 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675288 129783 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
49870810 129792 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675296 129792 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868783 129794 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675298 129794 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
58092273 129810 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675313 129810 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
66608367 124621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640808 124621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
50901935 131837 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694007 131837 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44397309 67528 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL189602 67528 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44417861 80626 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215113 80626 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424063 142073 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387989 142073 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
44388293 63285 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179260 63285 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425832 151476 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396221 151476 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
10257135 141651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424211 137184 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374843 137184 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279680 123588 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123588 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
45279871 123594 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123594 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279064 123595 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123595 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
25054804 19174 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289623 19174 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
49869492 128097 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665343 128097 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
49870553 129768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
10257135 141651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
11295707 168222 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL433591 168222 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416786 80299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 80299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
52947616 19139 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289399 19139 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44414368 141933 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL387055 141933 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424073 85625 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85625 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44437542 151725 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396447 151725 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437542 151725 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396447 151725 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
52947578 17045 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254556 17045 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
58092293 130417 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680177 130417 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
11610423 166019 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 166019 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
23567355 62407 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177981 62407 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
23567432 122619 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360303 122619 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
49868666 129662 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673559 129662 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
45278576 123586 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123586 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
2729098 80495 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80495 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
44417865 98192 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL274102 98192 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416559 79885 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212344 79885 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989356 168920 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL438637 168920 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416928 80599 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215040 80599 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
52947297 19231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290045 19231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44388219 63289 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179275 63289 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49869915 128112 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665358 128112 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
58093398 128143 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665388 128143 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
49870183 128157 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665401 128157 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
49869917 128158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665402 128158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
49869186 129786 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675290 129786 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL4115718 212904 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44417855 81392 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL215934 81392 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
44414319 141861 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386552 141861 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414392 80198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 80198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10347754 82458 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL217581 82458 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388289 63089 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178882 63089 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425809 97122 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL267690 97122 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44415389 81355 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 81355 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424253 85769 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229230 85769 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11634329 142300 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL388524 142300 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
10238912 75980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
11627316 140561 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381162 140561 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
10312052 141320 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL383432 141320 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
58423512 123581 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123581 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279871 123594 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123594 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45278578 123599 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123599 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
58423512 123581 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123581 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205152 19340 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290712 19340 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
44415389 81355 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 81355 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
49868938 128071 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665317 128071 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131828 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131828 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
49868676 128077 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665323 128077 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
11489588 80872 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215277 80872 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388427 63342 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179417 63342 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
23567283 63265 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179152 63265 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11656728 82272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217114 82272 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
49868674 128067 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665313 128067 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
50901934 131836 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694006 131836 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44424166 85919 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229929 85919 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44417833 82164 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216964 82164 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
45272120 196468 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563223 196468 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44416833 141595 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385038 141595 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424174 85804 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229556 85804 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
23567477 60510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175653 60510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44417881 80398 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214516 80398 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416839 81115 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215635 81115 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
49868937 128070 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665316 128070 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
44414522 96858 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL265365 96858 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10436862 79833 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212136 79833 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347753 80635 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215118 80635 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
45271246 195207 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550683 195207 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44414651 137231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL375132 137231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11340894 134590 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
CHEMBL371809 134590 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
49870457 128135 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665380 128135 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
49870809 129791 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675295 129791 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868781 129806 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675309 129806 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49868782 129807 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675310 129807 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902181 124628 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640817 124628 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
50903066 131827 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131827 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL4115726 212905 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416786 80299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 80299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
11641550 139733 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379829 139733 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
71714121 122549 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122549 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
44414357 79753 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79753 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430493 87009 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232438 87009 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44430500 87220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232835 87220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
9986014 141832 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386411 141832 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388294 63872 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL180364 63872 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397302 66941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL186642 66941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44415461 80301 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 80301 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415524 141216 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 141216 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44389404 122478 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360102 122478 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279772 123584 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123584 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
52941152 19189 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289723 19189 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
52947251 19204 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289830 19204 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
52941195 19217 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289946 19217 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
25017298 19305 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290493 19305 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16755970 92314 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 92314 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
44415524 141216 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 141216 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11467626 159808 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL410566 159808 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
49868803 128063 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665309 128063 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
44415461 80301 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 80301 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869073 128080 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665326 128080 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
49870553 129768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
44388263 165791 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL424784 165791 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
16756640 93278 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 93278 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
44416475 80407 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214547 80407 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45266975 194774 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
CHEMBL538211 194774 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
44417876 141722 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385743 141722 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
44416737 80494 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214717 80494 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44424203 166050 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL425669 166050 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44389484 62972 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178515 62972 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
44430490 86815 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232231 86815 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44437612 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437612 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437558 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437612 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437558 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437612 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91555 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91752 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437495 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44437495 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91900 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44424260 85778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229348 85778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
49868936 128069 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665315 128069 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870051 128164 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665408 128164 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
45267827 196235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561694 196235 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
44437609 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437609 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90961 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
49868668 129665 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673562 129665 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
58079421 129666 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673563 129666 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
66873457 128149 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665394 128149 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
66873578 128151 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 128151 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
57524507 126392 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651068 126392 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
57524583 126394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651070 126394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
66603668 129815 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675318 129815 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL4115747 212912 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414606 96734 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL264350 96734 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10348080 79800 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211984 79800 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347752 81095 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215567 81095 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430482 88363 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234930 88363 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44424171 85801 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229505 85801 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424179 85809 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229609 85809 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424182 85821 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229664 85821 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424255 142350 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388723 142350 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424181 142778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389274 142778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424185 168968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL439013 168968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44409479 75018 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
CHEMBL203388 75018 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
11699265 76732 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206637 76732 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
45279772 123584 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123584 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
45279321 123597 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123597 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45278578 123599 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123599 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45278577 123600 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123600 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194383 19303 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290491 19303 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25205149 19215 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289941 19215 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
137640352 156795 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL4071004 156795 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
16072132 80427 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214629 80427 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44414464 96820 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL265089 96820 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44409527 74872 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL203166 74872 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
50903065 131825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44417069 141913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
17989369 141769 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386050 141769 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10139496 169338 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL441855 169338 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44397323 67145 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187563 67145 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425796 86103 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231044 86103 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425821 143422 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389811 143422 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425801 86134 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231147 86134 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
49870683 129779 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675284 129779 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
44430481 151153 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395957 151153 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
20779441 63473 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179869 63473 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
45272111 195215 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550744 195215 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44416585 80270 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213923 80270 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416389 138653 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL377658 138653 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
58093337 128146 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
CHEMBL3665391 128146 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
58092304 129812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675315 129812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
58092269 130411 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680171 130411 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
44424061 85850 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229739 85850 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44417069 141913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414570 78039 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 78039 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
10008279 79798 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211978 79798 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10100662 141428 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384115 141428 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10461033 141442 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384163 141442 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388303 62550 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL178250 62550 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
44397350 125424 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL364573 125424 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
44425834 151416 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 151416 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415413 138376 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 138376 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
44424177 142003 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL387501 142003 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
25206616 18981 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1287838 18981 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
50903066 131827 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131827 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44415413 138376 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 138376 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
11168108 80419 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214583 80419 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415483 96415 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 96415 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869208 128083 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 128083 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
11656805 141844 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL386487 141844 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11648976 140336 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL380692 140336 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
11541231 141158 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL382772 141158 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
49870324 128118 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665363 128118 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
44388271 62977 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178549 62977 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
15982955 93648 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246794 93648 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
23567310 168501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL435329 168501 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
44437614 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
11786476 67233 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187942 67233 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
44437614 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 145137 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
25018075 19347 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290722 19347 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44416381 80148 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213383 80148 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44194482 19284 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290381 19284 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
44417885 80605 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215078 80605 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437541 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
49869779 128108 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665354 128108 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
58093367 128159 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665403 128159 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
57524675 126403 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
CHEMBL3651079 126403 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
66603581 130413 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680173 130413 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
58092191 124618 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640805 124618 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
50901932 131834 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3694004 131834 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
44417862 80631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
44414650 80200 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213649 80200 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44430478 87253 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 87253 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
44430452 149758 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149758 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
44430485 151443 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396193 151443 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415483 96415 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 96415 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11691468 169344 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL441886 169344 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
45278577 123600 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123600 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
52947270 19216 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289945 19216 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
49870553 129768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
25054550 19205 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289833 19205 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
49869489 128094 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665340 128094 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
49869632 128102 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
CHEMBL3665348 128102 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
44417837 141402 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383981 141402 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
44437541 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 146082 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
11445353 85141 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
CHEMBL224943 85141 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
3747253 94598 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
CHEMBL252145 94598 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
44437622 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437622 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 91376 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
45267809 196038 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560290 196038 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49870681 129773 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675279 129773 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44440599 146707 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL392403 146707 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
49870182 128166 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665410 128166 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44417841 81590 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81590 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44416782 80437 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80437 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44414455 80272 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 80272 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
44430498 88359 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234920 88359 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44424246 137563 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL375465 137563 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11655701 138708 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL377955 138708 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389403 63026 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178810 63026 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45278977 123582 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123582 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279680 123588 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123588 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
16756639 93230 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 93230 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
10195667 135288 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
CHEMBL372721 135288 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
44415533 79982 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79982 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 139335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 139335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425827 150911 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395763 150911 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415512 80350 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 80350 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
11504793 81570 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216209 81570 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397145 67387 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188766 67387 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10077022 17053 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254630 17053 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44424225 85777 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229339 85777 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44415512 80350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 80350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
45270416 196653 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL564409 196653 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44388058 166020 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
CHEMBL425521 166020 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
44437497 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437497 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91991 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424167 142114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388302 142114 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
67970877 126412 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
CHEMBL3651088 126412 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
49868917 129789 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
CHEMBL3675293 129789 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
49868914 129804 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129804 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092290 129808 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675311 129808 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902100 124630 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640819 124630 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
50903067 131828 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131828 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44424069 85730 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85730 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424064 85861 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229792 85861 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44414499 80327 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 80327 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
44430496 87116 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232634 87116 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397167 67238 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL187968 67238 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44425825 151201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395986 151201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415533 79982 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79982 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 139335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 139335 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
25205827 19260 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290262 19260 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
11247985 68026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL191390 68026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
44416782 80437 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80437 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44415526 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416714 141454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 141454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10300618 78378 18 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL2110360 78378 18 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
9954518 80028 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL212890 80028 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
10225681 80338 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214276 80338 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
17989329 81081 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215508 81081 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
16046114 141910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386925 141910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10159797 165979 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL425263 165979 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44397126 124274 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363479 124274 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11612847 82295 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
CHEMBL217182 82295 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
12020164 195753 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557473 195753 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416224 139498 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379457 139498 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
49869190 129802 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675305 129802 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
44424065 85862 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229793 85862 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
44416713 80464 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214667 80464 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45267812 196082 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560689 196082 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44424262 85779 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229350 85779 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
44416910 80516 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214790 80516 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
11387603 124267 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL363459 124267 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416711 80686 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215141 80686 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416579 81108 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215614 81108 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416817 169323 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL441696 169323 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
11569327 166004 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL425410 166004 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416881 82407 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 82407 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416800 96842 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96842 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11635674 201849 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL607121 201849 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11560835 139883 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379933 139883 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44414451 168939 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168939 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430460 87226 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 87226 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
11520239 3632 11 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
1313 3632 11 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
CHEMBL185271 3632 11 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
44396807 67101 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187371 67101 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
44397630 67370 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188654 67370 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397288 67446 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189043 67446 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
44397479 122049 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL359580 122049 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44424196 85868 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85868 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11569327 166004 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL425410 166004 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81566 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10165163 128506 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL366703 128506 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44414475 78075 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 78075 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424190 166174 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL426369 166174 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44388215 60718 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176079 60718 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10224210 63311 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179353 63311 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11353174 80597 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215030 80597 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416670 141924 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141924 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10128900 140901 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382140 140901 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756754 92129 27 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 92129 27 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
11610423 166019 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 166019 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
44424244 85759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229177 85759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11577410 76729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206616 76729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279402 123589 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123589 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45279868 123591 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123591 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
44416877 141394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 141394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
44481640 65477 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
CHEMBL1830049 65477 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
44424196 85868 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85868 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424256 168798 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL437544 168798 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279148 123593 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123593 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
50908739 19084 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289051 19084 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
10325618 92488 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243128 92488 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
10273126 61146 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176548 61146 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44417879 80383 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214470 80383 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
11584710 141300 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL383340 141300 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11524613 139233 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378869 139233 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44481905 65478 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830050 65478 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
10289615 77267 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL208025 77267 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
11584710 141300 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL383340 141300 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44417024 80389 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 80389 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416881 82407 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 82407 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416877 141394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 141394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10142124 60528 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175783 60528 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10164110 129475 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367215 129475 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414600 139527 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379535 139527 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11626170 79196 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
CHEMBL211340 79196 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
45279493 123579 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123579 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
24857598 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
24857598 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289283 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
50908738 19345 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1290720 19345 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
24857598 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289283 19121 16 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10165503 125953 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364871 125953 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
10115919 63358 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179493 63358 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11238080 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL205285 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414622 78088 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL210155 78088 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44424188 85849 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229716 85849 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11238080 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205285 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
44194850 19323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290601 19323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
44399610 67775 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67775 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11238080 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL205285 75967 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
44424194 85858 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229769 85858 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11504906 75870 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL204881 75870 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279489 123580 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123580 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
4033 1899 48 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
9826520 1899 48 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
CHEMBL214957 1899 48 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
25206454 19259 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290261 19259 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
11671178 76556 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206248 76556 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
16756074 92615 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
CHEMBL243578 92615 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
66873578 128151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 128151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
58092270 129772 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675278 129772 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
12020149 196494 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563412 196494 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455417 97461 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 97461 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
44425807 143414 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389808 143414 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425817 143421 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389810 143421 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424168 85932 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229983 85932 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424172 166172 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL426364 166172 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44389392 123084 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360977 123084 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
11238695 67596 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL190219 67596 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
10210351 122951 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360732 122951 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11317824 81543 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216068 81543 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44415525 81112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 81112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425793 86679 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL231651 86679 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
16756519 93015 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL244163 93015 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
44424072 85624 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85624 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44416650 80676 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215131 80676 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
10239389 127510 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL366161 127510 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
44437555 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44437555 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 169255 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44417880 141681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385535 141681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
23567391 63272 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179203 63272 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
45270386 195422 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552229 195422 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
15983865 93932 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
CHEMBL248267 93932 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
20877140 94574 7 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
CHEMBL251948 94574 7 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
49870326 128120 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665365 128120 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
67970575 126407 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651083 126407 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
49868916 129788 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675292 129788 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
58092271 129811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675314 129811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
50902096 124622 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640809 124622 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
16043220 78051 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL209964 78051 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416714 141454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 141454 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11612491 139870 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379927 139870 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
70695565 77989 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL2096889 77989 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430487 86714 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL231816 86714 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44415525 81112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 81112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424249 85767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229229 85767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424232 85918 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229926 85918 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279488 123574 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123574 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL4115701 212887 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
11169159 96795 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL264906 96795 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415526 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425818 161263 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412006 161263 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425790 142265 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL388491 142265 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44424236 85930 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL229980 85930 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
44437528 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437528 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 146206 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437524 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
44437524 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 146202 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
10239389 69330 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL192923 69330 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
11511638 76765 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL206813 76765 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
66873837 128127 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665372 128127 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870049 128162 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665406 128162 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
49868918 129798 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675301 129798 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
44415526 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
10392311 141766 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL386041 141766 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44415526 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 81091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415491 81111 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215621 81111 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424183 85811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229610 85811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10238912 75980 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75980 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389490 130670 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL368249 130670 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
25057124 19085 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289053 19085 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
50903069 131832 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693996 131832 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
15983730 169129 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL440229 169129 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44424176 194794 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL538652 194794 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44388077 166362 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
CHEMBL427484 166362 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
49868665 129661 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673558 129661 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
57524844 126411 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651087 126411 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
44417871 165939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL425084 165939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
10257298 141544 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384738 141544 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424178 166173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL426366 166173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
45279319 123332 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 123332 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25205320 19230 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290042 19230 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
16756637 93203 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 93203 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
44415402 141624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425812 161262 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412005 161262 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417849 96602 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL263296 96602 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
11282697 67263 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL188088 67263 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
45268694 196142 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
CHEMBL561148 196142 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
58580251 126418 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651707 126418 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
49870578 128139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665384 128139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
49869913 128110 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665356 128110 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
49869187 129799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675302 129799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49869189 129801 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675304 129801 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44414342 78036 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 78036 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414356 168918 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438615 168918 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44416261 79992 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212756 79992 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10099409 81126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215666 81126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10348749 96447 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL262175 96447 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415402 141624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
25205153 19202 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
CHEMBL1289824 19202 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
9848699 60638 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176024 60638 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
25056872 19206 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289834 19206 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
50903150 131826 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693990 131826 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
23567276 63181 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL178998 63181 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
44388355 62976 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178546 62976 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397312 67482 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189282 67482 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
49869074 128081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665327 128081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
49868799 129667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673564 129667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
57524674 126402 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651078 126402 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
50901933 131833 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3694003 131833 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44417869 80522 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214817 80522 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44424071 142097 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 142097 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
44414444 138607 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL377570 138607 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44454966 155426 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 155426 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44416753 141437 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 141437 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
10053890 79928 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212508 79928 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425798 153750 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398186 153750 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
17989409 80120 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL213255 80120 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
52948835 19154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289511 19154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25205316 19318 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290594 19318 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44416753 141437 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 141437 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416388 79811 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212032 79811 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416586 80374 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
CHEMBL214417 80374 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
21101402 141501 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL384489 141501 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
58092218 131831 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693995 131831 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
11410430 141815 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386311 141815 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415460 138141 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 138141 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44388265 122865 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL360567 122865 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44437557 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44437557 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91751 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44416472 80417 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214577 80417 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416428 81321 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL215898 81321 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
44416480 141777 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
CHEMBL386111 141777 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
44416816 80392 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
CHEMBL214504 80392 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
44416522 141399 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL383972 141399 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
44437525 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437525 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 91430 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437520 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437520 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
45272942 195681 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556661 195681 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49869776 124427 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3639642 124427 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
66874746 128152 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
CHEMBL3665397 128152 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
49868784 129809 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675312 129809 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
58092286 130415 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680175 130415 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
50902098 124626 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640815 124626 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
44430489 152856 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL397421 152856 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
10436663 166008 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425434 166008 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
44415460 138141 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 138141 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424233 85929 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229979 85929 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45278977 123582 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123582 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205321 19341 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290713 19341 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
10230235 131822 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL369392 131822 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44415462 80021 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 80021 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44440586 150829 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL395699 150829 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44417989 166171 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL426339 166171 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
10054046 17062 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254711 17062 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437498 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
12020169 194800 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
CHEMBL538711 194800 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
44437498 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147549 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870185 128116 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665361 128116 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
50902097 124623 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3640812 124623 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44417828 80681 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80681 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
11376122 81887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216471 81887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415462 80021 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 80021 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424199 85876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229875 85876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11635674 201849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 201849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756753 92128 1 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 92128 1 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
25206134 19081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289044 19081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
25205150 19214 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289940 19214 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 91202 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
50902099 124629 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640818 124629 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL4115716 212902 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414466 137476 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL375386 137476 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44414483 79733 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79733 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430499 87219 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232834 87219 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415446 161367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 161367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
45279319 123332 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 123332 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25017300 19287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290384 19287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16756186 93172 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 93172 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756521 93175 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244373 93175 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
44415446 161367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 161367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
44417863 80289 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214019 80289 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44415440 141753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425826 153747 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL398184 153747 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567290 63474 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179872 63474 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
20779442 63275 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179216 63275 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417831 80466 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
CHEMBL214670 80466 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
49868667 129664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673561 129664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
49870577 128138 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665383 128138 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
9799726 141874 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386660 141874 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414481 138900 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138900 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10256914 80173 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213491 80173 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415440 141753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424207 85933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229986 85933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692643 76551 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206195 76551 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
16755968 92492 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92492 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
1725351 126419 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
CHEMBL3651708 126419 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
49869629 128098 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665344 128098 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
44425823 143424 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389812 143424 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44539369 149355 1 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL3945242 149355 1 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
44424237 142505 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389059 142505 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16072132 80427 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80427 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
25110804 95490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95490 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44417024 80389 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 80389 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414309 138889 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138889 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430475 87070 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 87070 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430463 149399 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 149399 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
44397254 67301 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL188330 67301 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44397095 67548 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL189756 67548 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
44397018 123908 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL362790 123908 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397086 124271 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL363470 124271 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44396800 126809 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL365443 126809 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
16756073 92288 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 92288 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10310772 67778 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
CHEMBL190875 67778 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
44399610 67775 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67775 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11752750 60720 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60720 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911310 126421 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
CHEMBL3651710 126421 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
11340348 129460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367156 129460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414399 80923 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL215338 80923 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11511147 166195 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL426507 166195 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44388409 166239 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 166239 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
45279868 123591 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123591 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
25054013 19104 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289169 19104 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
11532924 138382 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 138382 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
11547011 141614 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141614 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
44424258 85774 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229291 85774 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11518999 140906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382177 140906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81566 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10203421 67459 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189147 67459 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
45279061 123592 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123592 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
25205319 19244 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290150 19244 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11548597 76225 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205838 76225 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279489 123580 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123580 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194749 19262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290265 19262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
44416895 80602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
46187172 121705 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3588863 121705 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
45279061 123592 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123592 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
52942456 19246 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
CHEMBL1290155 19246 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
16756187 93173 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 93173 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
16006978 80073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 80073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
71450863 78618 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL2112322 78618 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
25206612 19282 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290378 19282 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
16046124 80460 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80460 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416895 80602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80602 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416757 81149 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 81149 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
67970248 126408 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651084 126408 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL4115762 212925 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
45266979 194851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539737 194851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424261 144014 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL390288 144014 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
11526592 75031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL203445 75031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
25057913 19190 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289726 19190 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
20779426 60549 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
CHEMBL175874 60549 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
44425800 149326 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL394502 149326 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567408 168226 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL433608 168226 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
11330800 82274 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217132 82274 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388451 63497 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179974 63497 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11664134 82225 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217080 82225 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11519652 82469 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217618 82469 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
14514271 80481 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214684 80481 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
49870554 129769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675275 129769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
49869188 129800 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675303 129800 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
58092278 130416 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680176 130416 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
44455443 95711 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95711 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416629 80917 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL215321 80917 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44388425 63016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178755 63016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44424247 85760 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229178 85760 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424268 144018 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL390290 144018 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389406 62516 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178195 62516 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756522 93176 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL244374 93176 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
44416990 80964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
17989409 80120 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213255 80120 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44416479 80492 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
CHEMBL214715 80492 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
16110074 80581 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL214968 80581 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
17989406 82303 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217210 82303 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
18672590 141626 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385254 141626 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416627 80243 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL213817 80243 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44416738 80568 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL214916 80568 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44396904 66879 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL186338 66879 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
11385742 85073 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
CHEMBL224438 85073 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
45270393 195604 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL555875 195604 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424228 85873 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229870 85873 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44437516 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437516 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 91201 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44425806 97024 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266739 97024 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424266 85788 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229407 85788 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
44416798 80574 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL214941 80574 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
17989383 82466 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217610 82466 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44417859 80513 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214778 80513 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416990 80964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44397200 67372 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188659 67372 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11296279 80551 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214858 80551 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11410080 81136 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL215695 81136 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
49870580 128141 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665386 128141 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
57524585 126396 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651072 126396 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
66603270 130414 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680174 130414 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
44415459 78737 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78737 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
11698964 76325 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205874 76325 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
25054551 19175 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289624 19175 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
44415459 78737 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78737 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44415425 141456 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 141456 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44425804 86186 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231216 86186 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44397168 168276 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL433961 168276 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
57524843 126410 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651086 126410 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
46878210 201848 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607120 201848 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
49870811 129793 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675297 129793 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
9985881 80047 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212955 80047 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388365 63085 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178864 63085 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415425 141456 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 141456 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44424198 85869 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229824 85869 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424204 85920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229930 85920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
16756184 92139 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 92139 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
44425794 86680 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231652 86680 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425799 153751 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398187 153751 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
11698729 81541 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216066 81541 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397243 124378 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL363876 124378 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
15983733 93802 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247566 93802 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
2729502 81052 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 81052 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
45267015 194775 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL538215 194775 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416364 141445 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384172 141445 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10029835 141750 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385947 141750 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16756751 93310 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 93310 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
173712 124321 20 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL363548 124321 20 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
16756401 150942 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150942 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
52947025 17074 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254796 17074 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44416628 82481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL217699 82481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
45268725 196113 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
CHEMBL560953 196113 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
15983862 93845 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247764 93845 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44417839 161660 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL413051 161660 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
10325994 81079 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215501 81079 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
11353108 142113 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL388298 142113 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
16756403 150943 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150943 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
44416781 80435 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80435 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44440592 93696 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246992 93696 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
45272944 195696 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556868 195696 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
58092298 130412 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680172 130412 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
44397163 125053 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364414 125053 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10456385 92140 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 92140 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
10142464 128806 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL366934 128806 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
52941526 19140 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289400 19140 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44424169 143029 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL389483 143029 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424068 85750 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229092 85750 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
11786179 66839 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL186156 66839 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
50902182 124624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640813 124624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
11756387 141621 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385218 141621 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10098577 141896 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386819 141896 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415439 81452 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81452 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
1314 3727 21 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
9865843 3727 21 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
CHEMBL178707 3727 21 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
25017297 19304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290492 19304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44415439 81452 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81452 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11698276 82427 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217430 82427 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437547 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437547 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91747 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
20779429 60545 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175860 60545 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
50903068 131830 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131830 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44430486 86713 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL231815 86713 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415401 80262 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 80262 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16116777 66123 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL184037 66123 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416498 80144 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213370 80144 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416539 80234 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213767 80234 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
21101400 80300 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214081 80300 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416521 141398 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL383971 141398 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
11318577 68025 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
CHEMBL191388 68025 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
11678666 76709 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206498 76709 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
44415396 80166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 80166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
10160079 80102 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213171 80102 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
10277257 80401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214527 80401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989325 80844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215257 80844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416402 138571 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL377541 138571 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416781 80435 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80435 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44415466 140162 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 140162 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
9978490 122423 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 122423 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44417887 141484 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL384400 141484 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44424066 142074 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387990 142074 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
16046124 80460 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80460 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416757 81149 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 81149 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430471 86806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430459 87164 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 87164 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
44430468 92361 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 92361 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
44397245 67534 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189650 67534 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397293 124067 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363238 124067 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006978 80073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 80073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11706744 75540 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204407 75540 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
44417965 82147 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216820 82147 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
11376081 68032 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL191409 68032 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
11752750 60720 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60720 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911363 126423 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651712 126423 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
44414432 77938 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77938 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424206 168401 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL434747 168401 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10195637 76711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206503 76711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44424269 85795 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229461 85795 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44194954 19302 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290490 19302 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25017571 19324 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290602 19324 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44193792 19344 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290719 19344 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
56673836 65475 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
CHEMBL1830047 65475 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
10140707 63343 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179425 63343 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414318 80565 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214907 80565 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11684498 77651 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208845 77651 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424216 169328 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL441726 169328 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11678040 75459 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204212 75459 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279493 123579 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123579 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
44424193 142069 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387962 142069 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44194849 19261 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290264 19261 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
49836013 128124 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665369 128124 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
49868670 128082 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665328 128082 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
49869209 128084 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665330 128084 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
57383959 126398 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651074 126398 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
44414571 80275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 80275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279583 123590 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123590 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
25057388 19120 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289282 19120 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
25054288 19156 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289515 19156 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
11236807 81566 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81566 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10184368 63300 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179326 63300 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414375 80104 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213187 80104 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
45279583 123590 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123590 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
49869350 128093 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
CHEMBL3665339 128093 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
11454965 82514 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217761 82514 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11455871 141763 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL386035 141763 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44416405 141448 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 141448 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44481638 65479 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830051 65479 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
44462720 65480 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830052 65480 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
50908737 19137 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 19137 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44417840 81888 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
CHEMBL216472 81888 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
10304239 195826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL558277 195826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44415401 80262 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 80262 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425797 166329 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL427262 166329 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44415396 80166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 80166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415466 140162 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 140162 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11410594 97201 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL268385 97201 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416140 79793 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211964 79793 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415414 138680 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138680 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
45272984 195716 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL557070 195716 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416391 81533 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL216038 81533 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44440589 149092 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394310 149092 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44424067 143187 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 143187 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44415414 138680 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138680 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
49869211 128086 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665332 128086 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
44437522 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437522 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 91239 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437496 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437496 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91990 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44414552 80055 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL212979 80055 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416322 80504 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214750 80504 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44388311 63021 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178772 63021 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
16745305 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
16756524 143920 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL390212 143920 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
25057645 19191 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289727 19191 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
44415431 80065 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 80065 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
16745305 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 146380 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44388309 123287 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361423 123287 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
49870700 129660 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673557 129660 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
49870325 128119 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665364 128119 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
66873755 128174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665418 128174 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
44425803 97023 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266738 97023 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415431 80065 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 80065 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
44417868 80856 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215273 80856 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
58092274 129771 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675277 129771 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
9984325 96690 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL263975 96690 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430501 151188 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395979 151188 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44425837 86030 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230626 86030 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44416346 79858 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212230 79858 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389546 64773 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181931 64773 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45267814 196102 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560888 196102 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
44414601 138936 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL378439 138936 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44430488 86753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232027 86753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44416178 139894 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379940 139894 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424252 137567 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL375466 137567 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10229815 62336 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177900 62336 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL4115703 212889 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44389604 64292 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
CHEMBL181020 64292 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
45272117 195261 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL551149 195261 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49869774 128105 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
CHEMBL3665351 128105 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
57524506 126391 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
CHEMBL3651067 126391 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
58092289 129775 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
CHEMBL3675280 129775 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
66603252 129814 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675317 129814 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
44455367 95629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95629 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
16755967 92570 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243354 92570 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44415463 80022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 80022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 80009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 80009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415463 80022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 80022 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424205 85921 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229931 85921 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424173 143030 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
CHEMBL389484 143030 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
44389354 63936 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180658 63936 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
25017299 19325 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
CHEMBL1290603 19325 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
44415516 139292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 139292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 80009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 80009 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870679 129770 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675276 129770 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44417852 141659 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385393 141659 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
49868939 128072 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3665318 128072 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL4115761 212924 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44430484 86712 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL231814 86712 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415516 139292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 139292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16756404 92866 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244003 92866 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49869348 128090 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665336 128090 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49869349 128091 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665337 128091 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49870453 128123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665368 128123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
45270392 195036 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL549395 195036 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455414 97418 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 97418 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416801 80307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 80307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 97134 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 97134 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430455 86852 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86852 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430483 88373 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234931 88373 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44397497 67288 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL188206 67288 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
44397273 67468 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189190 67468 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44424187 85848 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229715 85848 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
25205318 19229 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290041 19229 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10137322 149408 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 149408 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44416801 80307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 80307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 97134 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 97134 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416405 141448 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 141448 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416390 141677 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141677 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44455444 95045 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 95045 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
11610423 166019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 166019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
44388227 60799 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL176142 60799 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
56660001 65474 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830046 65474 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424210 85752 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229112 85752 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
52941699 19138 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289396 19138 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25017033 19286 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19286 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
49869346 128088 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665334 128088 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
50903153 124620 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124620 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44389379 64634 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181776 64634 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279773 123585 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123585 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756642 93279 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 93279 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44414576 80038 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL212922 80038 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44414589 80164 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 80164 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424231 85917 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229925 85917 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
10186375 78948 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL2112988 78948 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
10141528 122950 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL360731 122950 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44388428 63307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179346 63307 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
1314 3727 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
9865843 3727 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
CHEMBL178707 3727 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
45279773 123585 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123585 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
11329623 82095 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216570 82095 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
52942796 19173 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289620 19173 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
11752320 67732 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL190780 67732 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
10206922 130704 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL368417 130704 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416390 141677 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141677 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44424189 142068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387961 142068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
49869491 128096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665342 128096 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
25205829 19245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290151 19245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11420621 67176 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL187721 67176 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
49870699 129659 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673556 129659 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
66873929 128173 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665417 128173 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
44388417 63222 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179072 63222 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11785261 67585 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67585 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
44430465 93299 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 93299 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
44425789 85949 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230080 85949 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16755872 92496 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92496 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
10185187 63299 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179325 63299 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44416553 79923 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
CHEMBL212487 79923 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
44416503 80388 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
CHEMBL214494 80388 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
17989373 80847 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215261 80847 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416606 81077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215493 81077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
44416502 168963 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
CHEMBL438966 168963 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
44416880 82449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44427407 142101 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
CHEMBL388234 142101 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
46911144 126420 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651709 126420 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
11273638 85149 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
CHEMBL225073 85149 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
44416880 82449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416580 141937 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL387081 141937 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
44416623 80420 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214584 80420 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44417878 141383 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383859 141383 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437519 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
12020152 195453 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552432 195453 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
16046157 141512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384548 141512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
44415427 80039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 80039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 140055 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 140055 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
44424265 144017 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
CHEMBL390289 144017 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
44415427 80039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 80039 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 140055 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 140055 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
11342100 85105 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224686 85105 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
10483729 16950 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253625 16950 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45269555 196119 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561011 196119 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44437519 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 91238 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44388314 130667 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL368228 130667 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
58093407 128142 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665387 128142 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
44415410 77934 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77934 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424184 85822 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229665 85822 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44415410 77934 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77934 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415426 141839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424175 85805 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229557 85805 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
25205493 19186 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289718 19186 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
10348147 80165 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213464 80165 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415426 141839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424170 85800 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229504 85800 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424250 85931 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229981 85931 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
45278576 123586 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123586 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756523 93201 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244576 93201 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
44437494 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437494 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424238 85756 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229164 85756 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44417829 80589 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215004 80589 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414506 141852 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386512 141852 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45268721 196739 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL565119 196739 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49870327 128121 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665366 128121 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414461 80250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL213840 80250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424270 85797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229463 85797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389509 62672 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178388 62672 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44417984 141824 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386354 141824 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
57524672 126400 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
CHEMBL3651076 126400 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
44437499 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437499 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91992 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870807 129778 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675283 129778 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
50902014 124619 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
CHEMBL3640806 124619 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
10029161 141891 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386759 141891 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
25018073 19346 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290721 19346 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44437523 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
44437523 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 146201 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
49868806 128068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665314 128068 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870050 128163 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665407 128163 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
49836011 129790 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675294 129790 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
44416862 81066 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 81066 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430453 87922 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87922 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
44425835 86016 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230521 86016 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425839 151228 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396008 151228 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16006976 82444 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82444 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424191 85856 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229767 85856 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11627700 82456 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217574 82456 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11452967 67529 1 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189611 67529 1 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
10140070 67624 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL190401 67624 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
49869212 128087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665333 128087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
25017572 19264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290267 19264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11329860 141682 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL385539 141682 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416862 81066 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 81066 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
49836016 129658 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
CHEMBL3673555 129658 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
49869210 128085 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665331 128085 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
66873757 128150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665395 128150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
9895005 139433 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379391 139433 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16006976 82444 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82444 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
50903153 124620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44481364 65481 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830053 65481 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
45279064 123595 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123595 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
45279062 123598 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123598 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
45279062 123598 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123598 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11168918 81661 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216368 81661 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
56666883 65471 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830043 65471 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44194853 19285 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290382 19285 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
11191656 141391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383901 141391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414654 80336 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214254 80336 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10077403 138931 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL378428 138931 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
58093324 128147 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665392 128147 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49869778 128107 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665353 128107 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
49870328 128122 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665367 128122 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49868678 128168 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665412 128168 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
44416607 165938 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165938 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44424197 143063 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL389517 143063 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11192044 77988 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL2096864 77988 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
44397103 124432 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363965 124432 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44437501 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
11641333 168743 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
CHEMBL437130 168743 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
44437501 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 154436 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44396985 124651 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364134 124651 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11720881 81878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216460 81878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11610423 166019 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 166019 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
67970371 126409 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651085 126409 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
57524762 126405 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
CHEMBL3651081 126405 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
44417860 80514 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL214779 80514 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
52942550 19299 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290484 19299 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44425820 97294 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL269061 97294 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44417870 80425 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214606 80425 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
10029836 81110 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215619 81110 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44396975 122254 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL359782 122254 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44416916 81409 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 81409 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416607 165938 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165938 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416561 80149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213386 80149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416664 82822 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
CHEMBL218030 82822 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
10295411 166137 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL426147 166137 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
11489282 144129 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL390377 144129 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
44415381 80576 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80576 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415381 80576 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80576 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415407 139440 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 139440 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
52944805 16951 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253626 16951 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437514 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437514 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 90345 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44389526 63249 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL179115 63249 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
44389375 64333 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181176 64333 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44425805 85972 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230307 85972 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415407 139440 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 139440 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11670645 85802 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229512 85802 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417854 80814 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215224 80814 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
16756638 93229 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 93229 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
52948254 17087 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254883 17087 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44417853 81539 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216056 81539 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44389378 64020 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180717 64020 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
50903154 131829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693993 131829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44388096 63510 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL180009 63510 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49870579 128140 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665385 128140 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
44416916 81409 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 81409 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430480 88362 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234929 88362 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
58092292 129781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675286 129781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49869327 129803 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675306 129803 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44417850 81657 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81657 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424070 85751 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85751 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44430477 87218 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 87218 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
10031575 139259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379002 139259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430476 152306 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 152306 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397087 67143 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187558 67143 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006977 140163 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 140163 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424180 142004 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL387502 142004 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692133 75430 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204161 75430 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
44194579 19118 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289278 19118 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
46911147 126422 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651711 126422 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
49868804 128065 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665311 128065 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
57524505 126390 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651066 126390 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
44414540 80326 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 80326 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
10217978 141086 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382631 141086 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
44399507 125170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
CHEMBL364500 125170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
11420203 67914 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL191078 67914 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
11752579 67915 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL191079 67915 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
122180707 121766 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3589155 121766 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
49869072 128078 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665324 128078 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
49869630 128100 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665346 128100 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
44414391 80197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 80197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424229 85874 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229871 85874 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
16718619 121765 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121765 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
52949941 19103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289166 19103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
49870323 128117 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665362 128117 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
49870455 128126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665371 128126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44389391 123083 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360976 123083 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
11156521 67228 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL187931 67228 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
49869912 128109 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665355 128109 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131828 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131828 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
10159789 60565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175943 60565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
16006977 140163 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 140163 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
58093333 128132 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665377 128132 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
16755969 92315 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 92315 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
49870181 128165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665409 128165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
44424192 85857 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229768 85857 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52947558 19119 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289279 19119 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
52941539 19155 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289512 19155 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
49869914 128111 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665357 128111 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
66874257 128154 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665399 128154 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
50903065 131825 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131825 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44224161 65472 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830044 65472 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424202 85878 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229877 85878 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52944997 19322 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290600 19322 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
11785262 69394 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69394 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
45279233 123601 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123601 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11752339 69399 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69399 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
44416989 80913 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80913 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430495 167638 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL430162 167638 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
16756402 92846 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92846 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
11409615 141765 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386039 141765 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
15983864 93931 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL248266 93931 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
52944068 19232 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290046 19232 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
58093391 128171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665415 128171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
57524584 126395 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651071 126395 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
57524587 126399 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651075 126399 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
44416287 139303 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL379201 139303 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
11577708 75556 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204514 75556 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL4115717 212903 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416311 80072 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213050 80072 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415467 80080 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 80080 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
49869777 128106 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665352 128106 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
44415467 80080 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 80080 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
50901936 131838 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
CHEMBL3694008 131838 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
44389422 168617 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL436081 168617 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
3575822 154343 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
CHEMBL398687 154343 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
3787955 154622 16 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
CHEMBL399303 154622 16 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
49870682 129780 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675285 129780 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
45278657 123576 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123576 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44437620 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44416172 78090 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL210167 78090 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44416225 138387 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377251 138387 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416966 141468 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL384302 141468 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
12020156 196282 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL562016 196282 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
44437620 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145689 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
67970689 126397 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651073 126397 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
44414542 80335 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 80335 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
4826270 94572 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
CHEMBL251946 94572 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
16116777 66123 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
CHEMBL184037 66123 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
44416554 79924 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
CHEMBL212488 79924 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
44416584 80269 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213922 80269 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416968 81538 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL216054 81538 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416495 141599 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL385054 141599 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
44416735 141625 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385253 141625 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
10277136 141865 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL386600 141865 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416841 80305 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214123 80305 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020168 194825 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539227 194825 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416174 141927 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL387025 141927 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416989 80913 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80913 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430494 87010 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232439 87010 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
16739310 86031 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230627 86031 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44425811 96990 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266513 96990 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415451 80056 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 80056 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11533835 76771 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206831 76771 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279488 123574 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123574 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58092287 129776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675281 129776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
44415451 80056 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 80056 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
66873669 128128 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665373 128128 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
11719877 85796 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229462 85796 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
16756752 142591 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142591 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
11260997 67244 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187996 67244 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
57524676 126404 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
CHEMBL3651080 126404 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
49869050 129797 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675300 129797 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49868915 129787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675291 129787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
11272081 81458 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215964 81458 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11590806 78317 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210926 78317 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
52941621 19203 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289829 19203 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
66898224 128131 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665376 128131 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49869048 129795 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
CHEMBL3675299 129795 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
49868780 129805 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675308 129805 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
44414649 139958 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379978 139958 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
16755971 92582 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL243507 92582 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
11691555 3788 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
1319 3788 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
CHEMBL384701 3788 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
44417835 82162 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216953 82162 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414528 138654 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
CHEMBL377664 138654 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
44388442 123122 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361139 123122 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
58093393 128148 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665393 128148 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424224 85771 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229285 85771 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424208 85934 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229988 85934 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279321 123597 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123597 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58093416 128130 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665375 128130 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414310 138482 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 138482 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
11785262 69394 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69394 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
49869633 128103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665349 128103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
66874268 128172 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665416 128172 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
11648753 140741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL381810 140741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424259 142400 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL388972 142400 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
11648753 140741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381810 140741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
11168186 68028 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 68028 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
11168186 68028 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
CHEMBL191393 68028 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
11489130 168224 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL433596 168224 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
44430479 170861 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL445407 170861 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
44424235 85622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL228289 85622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44425822 161264 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412007 161264 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44416689 81256 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215873 81256 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44417872 141786 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386163 141786 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
57524846 126414 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
CHEMBL3651090 126414 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
2276336 167678 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
CHEMBL430208 167678 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
44389405 63025 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178808 63025 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
17989439 93594 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246588 93594 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
10007632 80318 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214185 80318 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389440 62507 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
CHEMBL178147 62507 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
44388201 127819 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL366445 127819 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417061 97032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL266840 97032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425830 86029 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230625 86029 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756520 93174 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244372 93174 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44424267 85789 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229408 85789 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417836 82474 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL217653 82474 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
45279491 123575 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123575 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416173 141429 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384116 141429 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
45278657 123576 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123576 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44425802 143174 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389608 143174 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417842 82149 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216828 82149 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44480332 65476 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
CHEMBL1830048 65476 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
11752339 69399 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL193260 69399 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10239907 138735 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL378019 138735 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
45279233 123601 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123601 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
57524673 126401 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 126401 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
45279872 123596 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123596 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
66873409 128156 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665400 128156 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
11785261 67585 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67585 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
10297428 61983 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177426 61983 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
57524673 126401 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 126401 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
50903068 131830 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131830 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL4115702 212888 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
10415704 81146 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215728 81146 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
11613829 76455 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205979 76455 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
49869351 128092 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665338 128092 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
58093338 128133 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665378 128133 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44424209 137588 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL375520 137588 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
25057911 19157 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
CHEMBL1289516 19157 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
49869070 128075 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665321 128075 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
58093402 128169 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665413 128169 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
11511671 141208 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL382841 141208 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45279872 123596 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123596 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
11168186 68028 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 68028 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
66886732 128167 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665411 128167 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
58092272 129777 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675282 129777 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
50901931 131835 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694005 131835 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
11758499 157814 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL408332 157814 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424234 142504 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL389058 142504 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
24857597 19263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290266 19263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
9985634 79757 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79757 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870456 128136 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665381 128136 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
50903068 131830 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131830 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
49870048 128161 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665405 128161 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
44424254 85773 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229290 85773 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44397227 67167 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187660 67167 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
44416929 141439 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384156 141439 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
44425824 54816 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL161261 54816 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424200 85877 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229876 85877 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424201 143066 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL389518 143066 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11496824 81586 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216286 81586 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
44416275 81230 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL215850 81230 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44417891 80352 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214323 80352 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44425814 86085 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230940 86085 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
45272985 195717 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557071 195717 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
57524761 126406 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
CHEMBL3651082 126406 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
44437526 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44416223 139260 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379004 139260 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44437526 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 91431 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44389390 62946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178496 62946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
11642491 81582 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216267 81582 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437553 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437553 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 91145 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
50902011 131839 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694009 131839 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44409689 76769 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206825 76769 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
44389590 62510 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
CHEMBL178182 62510 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
11306487 67175 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
CHEMBL187719 67175 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
11202371 85080 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224519 85080 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
11192042 137349 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL375291 137349 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
50902015 124627 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640816 124627 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
44418000 141934 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL387065 141934 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
25206298 19283 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290379 19283 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
11520239 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3632 11 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1311 3446 0 None - 1 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
1295 3442 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
155817404 3442 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1298 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16167454 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16167454 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
91898993 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
91898993 2484 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1294 3441 0 None -1 2 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1294 3441 0 None 1 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1302 3975 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
155817405 3975 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1295 3442 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
155817404 3442 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1309 3444 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1308 3443 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1312 3527 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
16046160 3527 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
11238212 510 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1304 510 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1310 3445 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1291 765 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
268 765 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
11691555 3788 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1319 3788 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
CHEMBL384701 3788 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1297 3103 0 None - 1 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101600353 2470 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1301 2470 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
134824567 2470 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16207764 2470 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101110542 2471 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1293 2471 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101600353 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
101600353 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1301 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1301 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
134824567 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
134824567 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16207764 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16207764 2470 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101110542 2471 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1293 2471 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2484 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16167454 2484 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
91898993 2484 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073