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Ligand source activities (1 row/activity)

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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

CHEMBL3727412	135367	None	0	Human	Binding	Ki	=	134.00	6.87	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	534.2	7	1	6	4.66	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)CCc1ccc(Cl)cc1)CC2	-
CHEMBL3727434	135372	None	0	Human	Binding	Ki	=	6.00	8.22	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	554.2	5	1	7	4.38	C[C@H](Nc1nc2c(c(=O)n1N1CCCC1)CN(C(=O)c1ccc(C#N)cc1F)CC2)c1ccc(C(F)(F)F)cc1	-
CHEMBL3727443	135375	None	0	Human	Binding	Ki	=	10.00	8.00	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	492.1	5	1	7	4.06	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C)s1)CC2	-
CHEMBL3727469	135382	None	0	Human	Binding	Ki	=	6.00	8.22	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	527.2	7	1	8	3.33	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)COc1ccc(C#N)cc1)CC2	-
CHEMBL3727905	135454	None	0	Human	Binding	Ki	=	17.00	7.77	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	543.2	6	1	8	4.69	CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cccnc3s1)CC2	-
CHEMBL3728036	135471	None	0	Human	Binding	Ki	=	2.00	8.70	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	537.2	6	1	6	4.67	C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2	-
CHEMBL3728036	135471	None	0	Human	Binding	Ki	=	2.00	8.70	-	1	Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times.	ChEMBL	537.2	6	1	6	4.67	C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(C#N)cc1F)CC2	-
CHEMBL3728107	135484	None	0	Human	Binding	Ki	=	26.00	7.58	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	561.2	7	1	7	5.31	C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(-c3cnco3)cc1)CC2	-
CHEMBL3728107	135484	None	0	Human	Binding	Ki	=	26.00	7.58	-	1	Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times.	ChEMBL	561.2	7	1	7	5.31	C#CCCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(-c3cnco3)cc1)CC2	-
CHEMBL3728239	135509	None	0	Human	Binding	Ki	=	25.00	7.60	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	520.1	6	1	6	4.74	CCOn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2	-
CHEMBL3728315	135522	None	0	Human	Binding	Ki	=	9.00	8.05	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	529.1	5	1	8	4.30	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3cccnc3s1)CC2	-
CHEMBL3728379	135534	None	0	Human	Binding	Ki	=	6.00	8.22	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	498.2	6	1	6	4.33	C=Cc1ccc(C(=O)N2CCc3nc(N[C@@H](C)c4ccc(C(F)(F)F)cc4)n(OC)c(=O)c3C2)cc1	-
CHEMBL3728379	135534	None	0	Human	Binding	Ki	=	6.00	8.22	-	1	Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times.	ChEMBL	498.2	6	1	6	4.33	C=Cc1ccc(C(=O)N2CCc3nc(N[C@@H](C)c4ccc(C(F)(F)F)cc4)n(OC)c(=O)c3C2)cc1	-
CHEMBL3728578	135573	None	0	Human	Binding	Ki	=	121.00	6.92	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	554.1	7	1	6	5.30	COn1c(NC(CCC(F)(F)F)c2ccc(Cl)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2	-
CHEMBL3728578	135573	None	0	Human	Binding	Ki	=	121.00	6.92	-	1	Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times.	ChEMBL	554.1	7	1	6	5.30	COn1c(NC(CCC(F)(F)F)c2ccc(Cl)cc2)nc2c(c1=O)CN(C(=O)c1ccc(Cl)cc1)CC2	-
CHEMBL3728601	135576	None	0	Human	Binding	Ki	=	18.00	7.75	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	536.1	6	1	7	4.35	COc1cc(Cl)ccc1C(=O)N1CCc2nc(N[C@@H](C)c3ccc(C(F)(F)F)cc3)n(OC)c(=O)c2C1	-
CHEMBL3728776	135603	None	0	Human	Binding	Ki	=	15.00	7.82	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	530.2	5	1	7	3.11	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc3c(s1)=CCCC=3)CC2	-
CHEMBL3728824	135612	None	0	Human	Binding	Ki	=	24.00	7.62	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	545.2	5	1	6	5.21	CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2	-
CHEMBL3728824	135612	None	0	Human	Binding	Ki	=	24.00	7.62	-	1	Inhibition Assay: Receptor-expressing HEK 293 cell membrane fraction was analyzed by modifying the methods of C. J. Langmead et al. (see Langmead C J, Szekeres P G; Chambers J K, Ratcliffe S J, Jones D N C, Hirst W D, et al. Characterization of the binding of [125I]-human prolactin releasing peptide (PrRP) to GPR10, a novel G protein coupled receptor. Br J Pharmacol 2000; 131: 683-688.). To each well of a 96-well plate, 150 μl of assay buffer (20 mM HEPES, 10 mM EDTA, 1 μl/ml protease inhibiting agent cocktail, pH 7.4), 20 μl of cell membrane fraction, 10 μl of test compound and [3H]-PrRP (final concentration 1 nM) were added and incubated at room temperature for 90 minutes. After completion of the reaction, using a cell harvester, the cell-membrane fraction sample product was filtered under aspiration by a glass fiber filter plate (Unifilter; GF/B) previously treated with 0.5% polyethylene imine. The filter was washed with a 50 mM Tris hydrochloric acid buffer (pH 7.4) three times.	ChEMBL	545.2	5	1	6	5.21	CC#CCn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1ccc3ccccc3n1)CC2	-
CHEMBL3729024	135641	None	0	Human	Binding	Ki	=	20.00	7.70	-	1	Displacement of [3H]-PrRP from human GPR10 receptor expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method	ChEMBL	558.2	6	1	9	4.15	COn1c(N[C@@H](C)c2ccc(C(F)(F)F)cc2)nc2c(c1=O)CN(C(=O)c1cc(-c3cccs3)n(C)n1)CC2	-

Showing 1 to 20 of 190 entries

	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

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Ligand source activities (1 row/activity)