GPCRdb

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Ligand source activities (1 row/activity)

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Potency

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

BENZETHONIUM	11852	None	18	Human	Binding	Ki	=	3600.00	5.44	-8	35	Displacement of [125]metastin from metastin receptor	ChEMBL	412.3	11	0	2	6.07	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	https://dx.doi.org/10.1021/jm0609824
BENZETHONIUM	11852	None	18	Human	Binding	pKi	=	5.44	8.26	-8	35	Displacement of [125]metastin from metastin receptor	Drug Central	412.3	11	0	2	6.07	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	-
CHEMBL1163732	10438	None	0	Human	Binding	IC50	=	120.00	6.92	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	483.1	7	4	7	4.00	N#Cc1c(-c2ccc(C(=O)NCCN)cc2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163734	10439	None	0	Human	Binding	IC50	=	31.00	7.51	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	507.2	8	4	7	3.94	COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NCCN)c3)c2C#N)cc1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163735	10440	None	0	Human	Binding	IC50	=	15.00	7.82	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	495.2	7	4	7	4.30	CC(C)(CN)NC(=O)c1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3ccco3)c2C#N)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163736	10441	None	0	Human	Binding	IC50	=	8.00	8.10	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	485.1	7	4	7	3.67	N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163739	10442	None	0	Human	Binding	IC50	=	1200.00	5.92	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	481.2	7	4	7	4.43	Cc1c(-c2ccccc2O)nc(NC(=O)c2ccco2)c(C#N)c1-c1cccc(NC(=O)CCN)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163808	10444	None	0	Human	Binding	IC50	=	32.00	7.50	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	535.2	8	4	7	4.72	COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NC(C)(C)CN)c2)c1C#N	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163809	10445	None	0	Human	Binding	IC50	=	3.70	8.43	-	1	Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cells	ChEMBL	485.1	7	4	7	4.26	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.05.061
CHEMBL1163809	10445	None	0	Human	Binding	IC50	=	3.70	8.43	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	485.1	7	4	7	4.26	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163888	10447	None	0	Human	Binding	IC50	=	12.00	7.92	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	497.2	7	4	7	4.90	Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163896	10448	None	0	Human	Binding	IC50	=	9.80	8.01	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	517.1	7	4	7	5.25	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163897	10449	None	0	Human	Binding	IC50	=	19.00	7.72	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	561.0	7	4	7	5.36	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163972	10452	None	0	Human	Binding	IC50	=	120.00	6.92	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	507.2	8	4	7	4.54	COc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3ccccc3)n2)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164153	10455	None	0	Human	Binding	IC50	=	51.00	7.29	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	477.2	7	4	6	4.53	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164154	10456	None	0	Human	Binding	IC50	=	33000.00	4.48	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	483.1	7	4	7	4.00	N#Cc1c(-c2ccccc2C(=O)NCCN)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164235	10457	None	0	Human	Binding	IC50	=	1500.00	5.82	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	427.1	5	3	6	4.80	N#Cc1c(-c2cccc(CO)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164236	10458	None	0	Human	Binding	IC50	=	9900.00	5.00	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	441.1	5	3	6	5.00	N#Cc1c(-c2cccc(C(=O)O)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164603	10467	None	0	Human	Binding	IC50	=	2100.00	5.68	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	412.1	4	3	6	4.89	N#Cc1c(-c2cccc(N)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164673	10471	None	0	Human	Binding	IC50	=	570.00	6.24	-	1	Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	426.1	5	3	6	4.76	N#Cc1c(-c2cccc(CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036

Showing 1 to 20 of 284 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

4-fluorobenzoyl-FGLRW-NH2	117	None	0	Human	Functional	pEC50	=	-	9.20	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/18302161
[dY]¹KP-10	1520	None	0	Mouse	Functional	pIC50	=	-	8.40	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/19934405
CHEMBL1163736	10441	None	0	Human	Functional	IC50	=	660.00	6.18	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	485.1	7	4	7	3.67	N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163809	10445	None	0	Human	Functional	IC50	=	460.00	6.34	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	485.1	7	4	7	4.26	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163888	10447	None	0	Human	Functional	IC50	=	910.00	6.04	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	497.2	7	4	7	4.90	Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163896	10448	None	0	Human	Functional	IC50	=	4100.00	5.39	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	517.1	7	4	7	5.25	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1163897	10449	None	0	Human	Functional	IC50	=	6300.00	5.20	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	561.0	7	4	7	5.36	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164153	10455	None	0	Human	Functional	IC50	=	24000.00	4.62	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	477.2	7	4	6	4.53	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164674	10472	None	0	Human	Functional	IC50	=	1100.00	5.96	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	483.1	7	4	7	4.59	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1164939	10477	None	0	Human	Functional	IC50	=	1400.00	5.85	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	497.2	8	4	7	4.98	N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1165100	10479	None	0	Human	Functional	IC50	=	5100.00	5.29	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	483.1	7	4	7	4.00	N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1165222	10484	None	0	Human	Functional	IC50	=	3600.00	5.44	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	501.1	7	4	7	4.73	N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1165432	10491	None	0	Human	Functional	IC50	=	2500.00	5.60	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	527.2	8	4	7	4.69	CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1165783	10497	None	0	Human	Functional	IC50	=	2800.00	5.55	-	1	Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay	ChEMBL	469.1	6	4	7	4.20	N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1	https://dx.doi.org/10.1016/j.bmc.2010.04.036
CHEMBL1173643	10999	None	2	Human	Functional	IC50	=	930.00	6.03	-3	2	Antagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilization	ChEMBL	483.2	5	3	7	4.39	N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1	https://dx.doi.org/10.1016/j.bmc.2010.05.061
CHEMBL2151642	211748	None	0	Human	Functional	EC50	=	0.07	10.19	-3	2	Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis	ChEMBL	-	-	-	-	-	CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.08.069
CHEMBL2151643	80784	None	0	Human	Functional	EC50	=	0.04	10.39	9	2	Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis	ChEMBL	1331.6	38	19	16	-2.94	CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.08.069
CHEMBL2151644	80785	None	0	Human	Functional	EC50	=	0.62	9.21	2	2	Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis	ChEMBL	1301.7	39	19	16	-3.26	CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.08.069
CHEMBL2151645	80786	None	0	Human	Functional	EC50	=	0.95	9.02	4	2	Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis	ChEMBL	1315.6	38	19	16	-3.39	CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.08.069
CHEMBL2151646	80787	None	0	Human	Functional	EC50	=	0.05	10.30	-2	2	Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis	ChEMBL	1316.6	36	20	16	-3.64	CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.08.069

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